Publications
Publications
業績一覧
2018
‣Development of novel silanol-based human pregnane X receptor (PXR) agonists with improved receptor selectivity
Toyama, H., Shirakawa, H., Komai, M., Hashimoto, Y. and Fujii, S.:
Bioorg. Med. Chem. 15, 4493-4501 (2018).
‣Efficient lead finding, activity enhancement and preliminary selectivity control of nuclear receptor ligands bearing a phenanthridinone skeleton
Nishiyama, Y., Fujii, S., Makishima, M., Hashimoto, Y. and Ishikawa, M.:
Int. J. Mol. Sci. 19, 2090 (2018).
‣Design and synthesis of estrogen receptor ligands with a 4-heterocycle-4-phenylheptane skeleton.
Eto R, Misawa T, Noguchi-Yachide T, Ohoka N, Kurihara M, Naito M, Tanaka M and Demizu Y.:
Bioorg. Med. Chem. 26, 1638-1642 (2018).
‣Development of biotin-retinoid conjugates as chemical probes for analysis of retinoid function
Fujii, S., Mori, S., Kagechika, H., Mendoza, Parra MA. and Gronemeyer, H.:
Bioorg. Med. Chem. Lett. 28, 2442-2445 (2018).
‣Novel non-steroidal progesterone receptor (PR) antagonists with a phenanthridinone skeleton
Nishiyama, Y., Mori, S., Makishima, M., Fujii, S., Kagechika, H., Hashimoto, Y. and Ishikawa, M.:
ACS Med. Chem. Lett. 9, 641-645 (2018).
‣神経変性疾患原因タンパク質のケミカルノックダウン
石川稔、友重秀介、野村さやか、山下博子、大金賢司
MEDCHEM NEWS 28, 88-92 (2018).
‣Structural development of tetrachlorophthalimides as liver X receptor β (LXRβ)-selective agonists with improved aqueous solubility
Nomura, S., Endo-Umeda, K., Fujii, S., Makishima, M., Hashimoto, Y. and Ishikawa, M.:
Bioorg. Med. Chem. Lett. 28, 796-801 (2018).
‣Degradation of huntingtin mediated by a hybrid molecule composed of IAP antagonist linked to phenyldiazenyl benzothiazole derivative
Tomoshige, S., Nomura, S., Ohgane, K., Hashimoto, Y. and Ishikawa, M.:
Bioorg. Med. Chem. Lett. 28, 707-710 (2018).
2017
‣Structural basis for specific cleavage of Lys6-linked polyubiquitin chains by USP30
Sato, Y., Okatsu, K., Saeki, Y., Yamano, K., Matsuda, N., Kaiho, A., Yamagata, A., Goto-Ito, S., Ishikawa, M., Hashimoto, Y., Tanaka, K. and Fukai, S.:
Nat. Struct. Mol. Biol. 24, 911-919 (2017).
‣Affinity Labeling with 4-Azidophthalimide (AzPI): Relation between Labeling Rate and Fluorescence Intensity
Chiba, K., Hashimoto, Y. and Yamaguchi, T.:
Chem. Pharm. Bull. 65, 994-996 (2017).
‣Discovery of small molecules that induce degradation of huntingtin.
Tomoshige, S., Nomura, S., Ohgane, K., Hashimoto, Y. and Ishikawa, M.:
Angew. Chem. Int. Ed. 56, 11530-11533 (2017).
‣Photo-enhanced aqueous solubilization of an azo-compound.
Ishikawa, M., Ohzono, T., Yamaguchi, T. and Norikane, Y.:
Sci. Rep. 7, 6909 (2017).
‣1α-Hydroxy derivatives of 7-dehydrocholesterol are selective liver X receptor modulators
Endo-Umeda, K., Aoyama, A., Shimizu, M., Ishikawa, M., Hashimoto, Y., Yamada, S. and Makishima. M.:
J. Steroid Biochem. Mol. Biol. 172, 136-148 (2017).
‣Specific fluorescence labeling of target protein by using ligand–4-azidophthalimide conjugate.
Chiba, K., Asanuma, M., Ishikawa, M., Hashimoto, Y., Dodo, K., Sodeoka, M. and Yamaguchi, T.:
Chem. Commun. 53, 8751-8754 (2017).
‣Development of N6-(heteroarylcarbonyl)adenines as BRD4 inhibitors.
Amemiya, S., Yamaguchi, T., Hashimoto, Y. and Noguchi-Yachide, T.:
Heterocycles 94, 1107-1114 (2017).
‣Synthesis and evaluation of novel dual BRD4/HDAC inhibitors.
Amemiya, S., Yamaguchi, T., Hashimoto, Y. and Noguchi-Yachide, T.:
Bioorg. Med. Chem. 15, 3677-3684 (2017).
‣Switching subtype-selectivity: Fragment replacement strategy affords novel class of peroxisome proliferator-activated receptor α/δ (PPARα/δ) dual agonists.
Shioi, R., Okazaki, S., Noguchi-Yachide, T., Ishikawa, M., Makishima, M., Hashimoto, Y. and Yamaguchi, T.:
Bioorg. Med. Chem. Lett. 27, 3131-3134 (2017).
‣Development of nonsteroidal glucocorticoid receptor modulators based on N-benzyl-N-(4-phenoxyphenyl)benzenesulfonamide scaffold.
Yoshioka, H., Yamada, A., Nishiyama, Y., Kagechika, H., Hashimoto, Y. and Fujii, S.:
Bioorg. Med. Chem. 25, 3461-3470 (2017).
‣Structure-activity relationships of rosiglitazone for peroxisome proliferator-activated receptor gamma transrepression
Toyota, Y., Nomura, S., Makishima, M., Hashimoto, Y. and Ishikawa, M.:
Bioorg. Med. Chem. Lett. 27, 2776-2780 (2017).
‣Phenanthridin-6-one derivatives as the first class of non-steroidal pharmacological chaperones for Niemann-Pick disease type C1 protein.
Fukuda, H., Karaki, F., Dodo, K., Noguchi-Yachide, T., Ishikawa, M., Hashimoto, Y. and Ohgane, K.:
Bioorg. Med. Chem. Lett. 27, 2781-2787 (2017).
‣Progress in the medicinal chemistry of silicon: C/Si exchange and beyond.
Fujii, S. and Hashimoto Y.:
Future Med. Chem. 9, 485-505 (2017).
‣Structural Development Studies of Pyrazoloketone-Derived Acetyl-CoA Carboxylase Inhibitors.
Okazaki, S., Sakai, T., Ishikawa, M., Hashimoto, Y. and Yamaguchi, T.:
Heterocycles 95, 595-607 (2017).
‣Design and Synthesis of 1,3,5-Triazine Derivatives as Novel Inverse Agonists of Nuclear Retinoic Acid Receptor-Related Orphan Receptor-γ.
Kaitoh, K., Toyama, H., Hashimoto, Y. and Fujii, S.:
Heterocycles 95, 547-556 (2017).
‣Targeted degradation of proteins localized in subcellular compartments by hybrid small molecules.
Okuhira, K., Shoda, T., Omura, R., Ohoka, N., Hattori, T., Shibata, N., Demizu, Y., Sugihara, R., Ichino, A., Kawahara, H., Itoh, Y., Ishikawa, M., Hashimoto, Y., Kurihara, M., Itoh, S., Saito H. and Naito, M.:
Mol. Pharmacol. 91, 159-166 (2017).
2016
‣Development of N-(4-phenoxyphenyl)benzenesulfonamide derivatives as novel nonsteroidal progesterone receptor antagonists.
Yamada, A., Kazui, Y., Yoshioka, H., Tanatani, A., Mori, S., Kagechika, H. and Fujii, S.:
ACS Med. Chem. Lett. 7, 1028-1033 (2016).
‣Dichloromaleimide (diCMI): A Small and Fluorogenic Reactive Group for Use in Affinity Labeling.
Chiba, K., Hashimoto, Y. and Yamaguchi, T.:
Chem. Pharm. Bull. 64, 1647-1653 (2016).
‣Development of tetrachlorophthalimides as liver X receptor β (LXRβ)-selective agonists.
Nomura, S., Endo-Umeda, K., Makishima, M., Hashimoto, Y. and Ishikawa, M.:
ChemMedChem 11, 2347-2360 (2016).
‣Structure-activity relationship studies of non-carboxylic acid peroxisome proliferator-activated receptorα/δ (PPARα/δ) dual agonists.
Okazaki, S., Shioi, R., Noguchi-Yachide, T., Ishikawa, M., Makishima, M., Hashimoto, Y. and Yamaguchi, T.:
Bioorg. Med. Chem. 24, 5455-5461 (2016).
‣Discovery of N-(1-(3-(4-phenoxyphenyl)-1,2,4-oxadiazol-5-yl)ethyl)acetamides as novel acetyl-CoA carboxylase 2 (ACC2) inhibitors with peroxisome proliferator-activated receptor α/δ (PPARα/δ) dual agonistic activity.
Okazaki, S., Noguchi-Yachide, T., Sakai, T., Ishikawa, M., Makishima, M., Hashimoto, Y. and Yamaguchi, T.:
Bioorg. Med. Chem. 24, 5258-5269 (2016).
‣Isolation and characterization of hepatitis C virus resistant to a novel phenanthridinone derivative.
Ito, W., Toyama, M., Okamoto, M., Ikeda, M., Watashi, K., Wakita, T., Hashimoto, Y. and Baba M.:
Antivir. Chem. Chemother. 24, 148-154 (2015)
‣Structure-Activity Relationship Study of N(6)-Benzoyladenine-Type BRD4 Inhibitors and Their Effects on Cell Differentiation and TNF-α Production.
Amemiya, S., Yamaguchi, T., Sakai, T., Hashimoto, Y. and Noguchi-Yachide, T.:
Chem. Pharm. Bull. 64, 1378-1383 (2016).
‣Improvement in aqueous solubility of retinoic acid receptor (RAR) agonists by bending the molecular structure.
Hiramatsu, M., Ichikawa, Y., Tomoshige, S., Makishima, M., Muranaka, A., Uchiyama, M., Yamaguchi, T., Hashimoto, Y. and Ishikawa, M.:
Chem. Asian J. 11, 2210-2217 (2016).
‣Expanding the chemical space of hydrophobic pharmacophores: the role of hydrophobic substructures in the development of novel transcription modulators.
Fujii, S.:
Med. Chem. Commun. 7, 1082-1092 (2016).
‣BET Bromodomain as a Target of Epigenetic Therapy.
Noguchi-Yachide, T.:
Chem. Pharm. Bull. 64, 540-547 (2016).
‣Efficient protein knockdown of HaloTag-fused proteins using hybrid molecules consisting of IAP antagonist and HaloTag ligand.
Tomoshige, S., Hashimoto, Y. and Ishikawa, M.:
Bioorg. Med. Chem. 24, 3144-3148 (2016).
‣Altered activity profile of a tertiary silanol analog of multi-targeting nuclear receptor modulator T0901317.
Toyama, H., Sato, S., Shirakawa, H., Komai, M., Hashimoto, Y. and Fujii, S.:
Bioorg. Med. Chem. Lett. 26, 1817-1820 (2016).
2015
‣第9章 生命現象に関わる分子機構
長澤和夫,橋本祐一,村田道雄
大学院講義 有機化学 第2版 Ⅱ. 有機合成化学・生物有機化学, 野依良治・中筋一弘・玉尾浩平・奈良坂紘一・柴﨑正勝・橋本俊一・鈴木啓介・山本陽介・村田道雄編, pp407-437. 東京化学同人(東京)(2015).
‣Effects of alkyl side chains and terminal hydrophilicity on vitamin D receptor (VDR) agonistic activity based on the diphenylpentane skeleton.
Misawa, T., Yorioka, M., Demizu, Y., Noguchi-Yachide, T., Ohoka, N., Kurashima-Kinoshita, M., Motoyoshi, H., Nojiri, H., Kittaka, A., Makishima, M. Naito, M. and Kurihara, M.:
Bioorg. Med. Chem. Lett. 25, 5362-5366 (2015).
‣Degradation of HaloTag-fused nuclear proteins using bestatin-HaloTag ligand hybrid molecules.
Tomoshige, S., Naito, M., Hashimoto, Y., and Ishikawa, M.:
Org. Biomol. Chem. 13, 9746-9750 (2015).
‣Design and synthesis of 4-benzyl-1-(2H)-phthalazinone derivatives as novel androgen receptor antagonists.
Inoue, K., Urushibara, K., Kanai, M., Yura, K., Fujii, S., Ishigami-Yuasa, M., Hashimoto, Y., Mori, S., Kawachi, E., Matsumura, M., Hirano, T., Kagechika, H., and Tanatani, A.:
Eur. J. Med. Chem. 102, 310-319 (2015).
‣Styrylphenylphthalimides as novel transrepression-selective liver X receptor (LXR) modulators.
Nomura, S., Endo-Umeda, K., Aoyama, A., Makishima, M., Hashimoto, Y. and Ishikawa, M.:
ACS Med. Chem. Lett. 6, 902-907 (2015).
‣Discovery of non-competitive thrombin inhibitor derived from competitive tryptase inhibitor skeleton: Shift in molecular recognition resulted from skeletal conversion of carboxylate into phosphonate.
Aoyama, H., Ijuin, R., Kato, J., Urushiyama, S., Tetsuhashi, M., Hashimoto, Y., and Yokomatsu, T.:
Bioorg. Med. Chem. Lett. 25, 3676-3680 (2015).
‣Improving the Water-Solubility of Compounds by Molecular Modification to Disrupt Crystal Packing.
Ishikawa, M., and Hashimoto, Y.:
Chapter 31 in “The Practice of Medicinal Chemistry (Forth Edition)”, ed. by Camille Georges Wermuth, David Aldous, Pierre Raboisson and Didier Rognan, p747-765, Academic Press, Massachusetts, ISBN: 978-0-12-417205-0 (2015).
‣Design and synthesis of silicon-containing fatty acid amide derivatives as novel peroxisome proliferator-activated receptor (PPAR) agonists.
Kajita, D., Nakamura, M., Matsumoto, Y., Ishikawa, M., Hashimoto, Y., and Fujii, S.:
Bioorg. Med. Chem. Lett. 25, 3350-3354 (2015).
‣Design and synthesis of novel ROR inverse agonists with a dibenzosilole scaffold as a hydrophobic core structure
Toyama, H., Nakamura, M., Hashimoto, Y., and Fujii, S.:
Bioorg. Med. Chem. 23, 2982-2988 (2015).
‣Structure-Activity Relationships of Benzhydrol Derivatives Based on 1'-Acetoxychavicol Acetate (ACA) and their Inhibitory Activities on Multiple Myeloma Cell Growth via Inactivation of the NF-kB Pathway.
Misawa, T., Dodo, K., Ishikawa, M., Hashimoto, Y., Sagawa, M., Kizaki, M., and Aoyama, H.:
Bioorg. Med. Chem. 23, 2241-2246 (2015).
‣Synthesis of new hydantoins bearing glutarimide or succinimide moiety and their evaluation for cell differentiation-inducing and anti-angiogenic activities.
Yamaguchi, J., Noguchi-Yachide, T., Sakaguchi, Y., Shibata, C., Kanuma, S., Yoshizaki, A., Takizawa, Y., and Hashimoto, Y.:
Heterocycles 91, 764-781 (2015).
‣TM-233, a novel analog of ACA, induces cell death in myeloma cells by inhibiting both JAK/STAT and proteasome activities.
Sagawa, M., Tabayashi, Y., Kimura, Y., Tomikawa, T., Nemoto, T., Watanabe, R., Tokuhira, M., Ri, M., Hashimoto, Y., Iida, S., and Kizaki, M.:
Cancer Sci. 106, 438-446 (2015)
‣Discovery and structure-activity relationship studies of N6-benzoyladenine derivatives as novel BRD4 inhibitors.
Noguchi-Yachide, T., Sakai, T., Hashimoto, Y., and Yamaguchi, T.:
Bioorg. Med. Chem. 23, 953-959 (2015).
‣Design, synthesis and structure-activity relationship studies of novel sirtuin 2 (SIRT2) inhibitors with a benzamide skeleton.
Sakai, T., Matsumoto, Y., Ishikawa, M., Sugita, K., Hashimoto, Y., Wakai, N., Kitao, A., Morishita, E., Toyoshima, C., Hayashi, T., and Akiyama, T.:
Bioorg. Med. Chem. 23, 328-339 (2015).
2014
‣Development of 2-thioxoquinazoline-4-one derivatives as dual and selective inhibitors of dynamin-related protein 1 (Drp1) and puromycin-sensitive aminopeptidase (PSA).
Numadate, A., Mita, Y., Matsumoto, Y., Fujii, S., and Hashimoto, Y.:
Chem. Pharm. Bull. 62, 979-988 (2014).
‣Structure-activity relationships of oxysterol-derived pharmacological chaperones for Niemann-Pick type C1 protein.
Ohgane, K., Karaki, F., Noguchi-Yachide, T., Dodo, K., and Hashimoto, Y.:
Bioorg. Med. Chem. Lett. 24, 3480-3485 (2014).
‣Structure-activity relationship study of non-steroidal NPC1L1 ligands identified through cell-based assay using pharmacological chaperone effect as a readout.
Karaki, F., Ohgane, K., Fukuda, H., Nakamura, M., Dodo, K., and Hashimoto, Y.:
Bioorg. Med. Chem. 22, 3587-3609 (2014).
‣A Novel Tetramethylnaphthalene Derivative Selectively Inhibits Adult T-Cell Leukemia (ATL) Cells In Vitro.
Toyama, M., Aoyama, H., Mukai, R., Nakamura, M., Yoshimura, K., Okamoto, M., Ohshima, T., Hashimoto, Y., and Baba, M.:
Anticancer Res. 34, 1771-1778 (2014).
‣Structure-activity relationship-guided development of retinoic acid receptor-related orphan receptor gamma (RORγ)-selective inverse agonists with a phenanthridin-6(5H)-one skeleton from a liver X receptor ligand.
Nishiyama, Y., Nakamura, M., Misawa, T., Nakagomi, M., Makishima, M., Ishikawa, M., and Hashimoto, Y.:
Bioorg. Med. Chem. 22, 2799-2808 (2014).
‣Design and synthesis of silicon-containing steroid sulfatase inhibitors possessing pro-estrogen antagonistic character.
Kajita, D., Nakamura, M., Matsumoto, Y., Makishima, M., and Hashimoto Y.:
Bioorg. Med. Chem. 22, 2244−2252 (2014).
‣Development of novel silicon-containing inverse agonists of retinoic acid receptor-related orphan receptors.
Toyama, H., Nakamura, M., Nakamura, M., Matsumoto, Y., Nakagomi, M., and Hashimoto Y.:
Bioorg. Med. Chem. 22, 1948-1959 (2014).
‣7-Dehydrocholesterol metabolites produced by sterol 27-hydroxylase(CYP27A1) modulate liver X receptor activity.
Endo-Umeda, K., Yasuda, K., Sugita, K., Honda, A., Ohta, M., Ishikawa, M., Hashimoto, Y., Sakaki, T., and Makishima, M.:
J. Steroid Biochem. Mol. Biol. 140, 7–16 (2014).
2013
‣Design and synthesis of silicon-containing tubulin polymerization inhibitors: Replacement of the ethylene moiety of combretastatin A-4 with a silicon linker.
Nakamura, M., Kajita, D., Matsumoto, Y., and Hashimoto, Y.:
Bioorg. Med. Chem. 21, 7381-7391 (2013).
‣タンパク質の折り畳みの異常を直すファーマコロジカルシャペロン ーニーマンピック病C型治療薬を目指した取組みー
大金賢司、唐木文霞、どど孝介、橋本祐一:
現代化学 512, 48-54 (2013).
‣Structure-activity relationship studies of Niemann-Pick type C1-like 1 (NPC1L1) ligands identified by screening assay monitoring pharmacological chaperone effect.
Karaki, F., Ohgane, K., Dodo, K., and Hashimoto, Y.:
Bioorg. Med. Chem. 21, 5297-5309 (2013).
‣Structure–activity relationships of bisphenol A analogs at estrogen receptors (ERs): Discovery of an ERα-selective antagonist.
Maruyama, K., Nakamura, M., Tomoshige, S., Sugita, K., Makishima, M., Hashimoto, Y. and Ishikawa, M.:
Bioorg. Med. Chem. Lett. 23, 4031-4036 (2013).
‣分子構造の非平面化・非対称化による溶解度向上策と創薬化学への応用
石川稔、橋本祐一:
有機合成化学協会誌 71, 625-636 (2013).
‣Synthesis and evaluation of 2,3-dinorprostaglandins: Dinor-PGD1 and 13-epi-dinor-PGD1 are peroxisome proliferator-activated receptor α/γ dual agonists.
Sato, A., Dodo, K., Makishima, M., Hashimoto, Y. and Sodeoka, M.:
Bioorg. Med. Chem. Lett. 23, 3013-3017 (2013).
‣Discovery of Oxysterol-Derived Pharmacological Chaperones for NPC1: Implication for the Existence of Second Sterol-Binding Site
Ohgane, K., Karaki, F., Dodo, K. and Hashimoto, Y.:
Chem. Biol. 20, 391-402 (2013).
‣Development of silicon-containing bis-phenol derivatives as androgen receptor antagonists: Selectivity switching by C/Si exchange
Nakamura, M., Makishima, M. and Hashimoto, Y.:
Bioorg. Med. Chem. 21, 1643-1651 (2013).
‣Organosilicon Compounds as Adult T-Cell Leukemia Cell Proliferation Inhibitors.
Nakamura, M., Matsumoto, Y., Toyama, M., Baba, M. and Hashimoto, Y.:
Chem. Pharm. Bull. 61, 237–241 (2013).
‣Structure–activity relationship of benzodiazepine derivatives as LXXLL peptide mimetics that inhibit the interaction of vitamin D receptor with coactivators.
Mita, Y., Dodo, K., Noguchi-Yachide, T., Hashimoto, Y. and Ishikawa, M.:
Bioorg. Med. Chem. 21, 993-1005 (2013).
‣Small-molecular, non-peptide, non-ATP-competitive polo-like kinase 1 (Plk1) inhibitors with a terphenyl skeleton.
Mita, Y., Noguchi-Yachide, T., Ishikawa, M. and Hashimoto, Y.:
Bioorg. Med. Chem. 21, 608-617 (2013).
2012
‣Riccardin C derivatives as anti-MRSA agents: Structure-activity relationship of a series of hydroxylated bis(bibenzyl)s.
Sawada, H., Okazaki, M., Morita, D., Kuroda, T., Matsuno, K., Hashimoto, Y. and Miyachi, H.:
Bioorg. Med. Chem. Lett. 22, 7444-7447 (2012).
‣Specific Inhibitors of Puromycin-Sensitive Aminopeptidase with a 3-(Halogenated Phenyl)-2,4(1H,3H)-quinazolinedione Skeleton
Matsumoto, Y., Noguchi-Yachide, T., Nakamura, M., Mita, Y., Numadate, A. and Hashimoto, Y.:
Heterocycles 86, 1449-1463 (2012).
‣Small-molecular inhibitors of Ca2+-induced mitochondrial permeability transition (MPT) derived from muscle relaxant dantrolene
Murasawa, S., Iuchi, K., Sato, S., Noguchi-Yachide, T., Sodeoka, M., Yokomatsu, T., Dodo, K., Hashimoto, Y. and Aoyama, H.:
Bioorg. Med. Chem. 20, 6384-6393 (2012).
‣Design, synthesis and in vitro evaluation of a series of α-substituted phenylpropanoic acid PPARγ agonists to further investigate the stereochemistry–activity relationship
Ohashi, M., Nakagome, I., Kasuga, J., Nobusada, H., Matsuno, K., Makishima, M., Hirono, S., Hashimoto, Y. and Miyachi, H.:
Bioorg. Med. Chem. 20, 6375-6383 (2012).
‣生体有機化学
橋本祐一、村田道雄 編著
東京化学同人、東京、(2012)
‣Design, synthesis, and biological evaluation of novel transrepression-selective liver X receptor (LXR) ligands with 5,11-dihydro-5-methyl-11-methylene-6Hdibenz[b,e]azepin-6-one skeleton
Aoyama, A., Endo-Umeda, K., Kishida, K., Ohgane, K., Noguchi-Yachide, T., Aoyama, H., Ishikawa, M., Miyachi, H., Makishima, M. and Hashimoto, Y.:
J. Med. Chem. 55, 7360-7377 (2012).
‣Synergistic inhibition of HTLV-1-infected cell proliferation by combination of cepharanthine and a tetramethylnaphthalene derivative.
Toyama, M., Hamasaki, T., Uto, T., Aoyama, H., Okamoto, M., Hashimoto, Y. and Baba, M.:
Anticancer Res. 32, 2639-2646 (2012).
‣Double protein knockdown of cIAP1 and CRABP-II using a hybrid molecule consisting of ATRA and IAPs antagonist
Itoh, Y., Ishikawa, M., Kitaguchi, R., Okuhira, K., Naito, M. and Hashimoto, Y.:
Bioorg. Med. Chem. Lett. 22, 4453-4457 (2012).
‣E297G mutated bile salt export pump (BSEP) function enhancers derived from GW4064: Structural development study and separation from farnesoid X receptor-agonistic activity.
Misawa, T., Hayashi, H., Makishima, M., Sugiyama, Y. and Hashimoto, Y.:
Bioorg. Med. Chem. Lett. 22, 3962-3966 (2012).
‣Bidirectional fluorescence properties of pyrene-based peroxisome proliferator-activated receptor (PPAR) α/δ dual agonist.
Ban, S., Oyama, T., Kasuga, J., Ohgane, K., Nishio, Y., Morikawa, K., Hashimoto, Y. and Miyachi, H.:
Bioorg. Med. Chem. 20, 3460-3464 (2012).
‣Discovery and structural development of small molecules that enhance transport activity of bile salt export pump mutant associated with progressive familial intrahepatic cholestasis type 2
Misawa, T., Hayashi, H., Sugiyama, Y. and Hashimoto, Y.:
Bioorg. Med. Chem. 20, 2940-2949 (2012).
‣フォールディング異常症に対する治療薬創製の可能性
橋本祐一:
MEDCHEM NEWS 22(1), 25-28 (2012).
2011
‣Potent and selective inhibition of hepatitis C virus replication by novel phenanthridinone derivatives
Salim, M.T., Aoyama, H., Sugita, K., Watashi, K., Wakita, T., Hamasaki, T., Okamoto, M., Urata, Y. Hashimoto, Y. and Baba, M.:
Biochem. Biophys. Res. Commun. 415, 714-719 (2011).
‣Confirmation of Molecular Planarity Disruption Effect on Aqueous Solubility Improvement of β-Naphthoflavone Analogs.
Fujita, Y., Yonehara, M., Kitahara, K., Shimokawa, J., Hashimoto, Y. and Ishikawa, M.:
Heterocycles 83, 2563-2575 (2011).
‣Design, Synthesis and Biological Evaluation of Nuclear Receptor-degradation Inducers
Itoh, Y., Kitaguchi, R., Ishikawa, M., Naito, M. and Hashimoto, Y.:
Bioorg. Med. Chem. 19, 6768-6778 (2011).
‣Estrogen Receptor α/β Ligands Derived from Thalidomide.
Noguchi-Yachide, T., Sugita, K. and Hashimoto, Y.:
Heterocycles 83, 2137-2147 (2011).
‣Selective Inhibition of HTLV-1-infected Cell Proliferation by a Novel Tetramethylnaphthalene Derivative.
Hamasaki, T., Toyama, M., Aoyama, H., White, Y., Okamoto, M., Arima, N., Hashimoto, Y. and Baba, M.:
Anticancer Res. 31, 2241-2247 (2011).
‣Inhibition of restriction enzymes EcoRI, BamHI and HindIII by phenethylphenylphthalimides derived from thalidomide.
Motoshima, K., Ishikawa, M., Hashimoto, Y. and Sugita, K.:
Chem. Pharm. Bull. 59, 880-884 (2011).
‣Development of Target Protein-Selective Degradation Inducer for Protein Knockdown.
Itoh, Y., Ishikawa, M., Kitaguchi, R., Sato, S., Naito, M. and Hashimoto, Y.:
Bioorg. Med. Chem. 19, 3229-3241 (2011).
‣Structure-based design, synthesis, and nonalcoholic steatohepatitis (NASH)-preventive effect of phenylpropanoic acid peroxisome proliferator-activated receptor (PPAR) α-selective agonists.
Ban, S., Kasuga, J., Nakagome, I., Nobusada, H., Takayama ,F., Hirono, S., Kawasaki, H., Hashimoto, Y. and Miyachi H.:
Bioorg Med Chem. 19, 3183-3191 (2011).
‣Peroxisome proliferator-activated receptor agonists with phenethylphenylphthalimide skeleton derived from thalidomide-related liver X receptor antagonists:Relationship between absolute configuration and subtype selectivity.
Motoshima, K., Ishikawa, M., Hashimoto, Y. and Sugita, K.:
Bioorg. Med. Chem. 19, 3156-3172 (2011).
‣Non-competitive and selective dipeptidyl peptidase IV inhibitors with phenethylphenylphthalimide skeleton derived from thalidomide-related α-glucosidase inhibitors and liver X receptor antagonists.
Motoshima, K., Sugita, K., Hashimoto, Y. and Ishikawa, M.:
Bioorg. Med. Chem. Lett. 21, 3041-3045 (2011).
‣Fused heterocyclic amido compounds as anti-hepatitis C virus agents.
Aoyama, H., Sugita, K., Nakamura, M., Aoyama, A., Salim, M.T., Okamoto, M., Baba, M. and Hashimoto, Y.:
Bioorg. Med. Chem. 19, 2675-2687 (2011).
‣Specific degradation of CRABP-II via cIAP1-mediated ubiquitylation induced by hybrid molecules that crosslink cIAP1 and the target protein.
Okuhira, K., Ohoka, N., Sai, K., Nishimaki-Mogami, T., Itoh, Y., Ishikawa, M., Hashimoto, Y. and Naito, M.:
FEBS Lett. 585, 1147–1152 (2011).
‣Improvement in aqueous solubility in small molecule drug discovery programs by disruption of molecular planarity and symmetry.
Ishikawa, M. and Hashimoto, Y.:
J. Med. Chem. 54, 1539-1554 (2011).
‣Structural Development Study of a Novel Pharmacological Chaperone for Folding-defective Rhodopsin Mutants Responsible for Retinitis Pigmentosa.
Ohgane, K., Dodo, K. and Hashimoto Y.:
Yakugaku Zasshi 131, 325-334 (2011).
‣Further Application of the Multi-Template Approach for Creation of Biological Response Modifiers: Discovery of a New Class of Multifunctional Anti-Diabetic Agents.
Motoshima, K., Noguchi-Yachide, T., Ishikawa, M., Hashimoto, Y. and Sugita, K.:
Heterocycles 82, 1083-1101 (2011).
‣Design, synthesis and structural analysis of phenylpropanoic acid-type PPARγ-selective agonists: discovery of reversed stereochemistry-activity relationship.Mast cell death induced by 24(S),25-epoxycholesterol.
Ohashi, M., Ohyama, T., Nakagome, I., Satoh, M., Nishio, Y., Hirono, S., Morikawa, K., Hashimoto Y. and Miyachi, Y.:
J. Med. Chem. 54, 331-341 (2011).
‣ビタミンD受容体−コアクチベーター相互作用阻害物質の創製.
三田裕介、橋本祐一、石川稔:
ビタミン 85, 25-26 (2011).
2010
‣Mast cell death induced by 24(S),25-epoxycholesterol.
Fukunaga, M., Nunomura, S., Nishida, S., Endo, K., Gon, Y., Hashimoto, S., Hashimoto, Y., Okayama, Y., Makishima, M. and Ra, C.:
Experimental Cell Res. 316, 3272-3281 (2010).
‣Highly potent and selective inhibition of bovine viral diarrhea virus replication by γ-carboline derivatives.
Salim, M.T., Goto, Y., Hamasaki, T., Okamoto, M., Aoyama, H., Hashimoto, Y., Musiu, S., Paeshuyse, J., Neyts, J., Froeyen, M., Herdewijn, P. and Baba, M.:
Antiviral Res. 88, 263-268 (2010).
‣Design and synthesis of phthalimide-based fluorescent liver X receptor antagonists.
Kishida, K., Aoyama, A., Hashimoto, Y. and Miyachi, H.:
Chem. Pharm. Bull. 58, 1525-1528 (2010).
‣Novel Selective Anti-androgens with a Diphenylpentane Skeleton.
Maruyama, K., Noguchi-Yachide, T., Sugita, K., Hashimoto, Y. and Ishikawa, M.:
Bioorg. Med. Chem. Lett. 20, 6661-6666 (2010).
‣Improvement of water-solubility of biarylcarboxylic acid peroxisome proliferator-activated receptor (PPAR) δ-selective partial agonists by disruption of molecular planarity/symmetry.
Kasuga, J., Ishikawa, M., Yonehara, M., Makishima, M., Hashimoto, Y. and Miyachi, H.:
Bioorg. Med. Chem. 18, 7164-7173 (2010).
‣Retinobenzaldehydes as proper-trafficking inducers of folding-defective P23H rhodopsin mutant responsible for Retinitis Pigmentosa.
Ohgane, K., Dodo, K. and Hashimoto, Y.:
Bioorg. Med. Chem. 18, 7022-7028 (2010).
‣γ-Carboline derivatives as potent and selective inhibitors of bovine viral diarrhea virus (BVDV) replication.
Baba, M., Salim, M.T., Okamoto, M., Aoyama, H., Hashimoto, Y., Takebe, Y., Paeshuyse, J. and Neyts, J.:
Antiviral Res. 86, A29 (2010).
‣Anti-influenza activity of phenethylphenylphthalimide analogs derived from thalidomide.
Iwai, Y., Takahashi, H., Hatakeyama, D., Motoshima, K., Ishikawa, M., Sugita, K., Hashimoto, Y., Harada, Y., Itamura, S., Odagiri, T., Tashiro, M., Sei, Y., Yamaguchi Y. and Kuzuhara, T.:
Bioorg. Med. Chem. 18, 5379-5390 (2010).
‣Development of tryptase inhibitors derived from thalidomide.
Tetsuhashi, M., Ishikawa, M., Hashimoto, M., Hashimoto, Y. and Aoyama, H.:
Bioorg. Med. Chem. 18, 5323-5338 (2010).
‣Synthesis and anti-hepatitis C virus activity of morpholino triazine derivatives.
Misawa, T., Salim, M.T., Okamoto, M., Baba, M., Aoyama, H. Hashimoto, Y. and Sugita, K.:
Heterocycles 81, 1419-1426 (2010).
‣Nitrogen-containing fused-heteroaromatic compounds as anti-bovine diarrhea virus (BVDV) agents. Aoyama, H., Baba, M. and Hashimoto, Y.:
Curr. Bioactive Comp. 6, 118-128 (2010).
‣Anti-bovine viral diarrhoea virus activity of novel diphenylmethane derivatives.
Salim, M.T., Okamoto, M., Hosoda, S., Aoyama, H., Hashimoto Y. and Baba, M.:
Antiviral Chem. Chemother. 20, 193-200 (2010).
‣Protein Knockdown Using Methyl Bestatin-ligand Hybrid Molecules: Design and Synthesis of Inducers of Ubiquitination-mediated Degradation of Cellular Retinoic Acid-Binding Proteins.
Itoh, Y., Ishikawa, M., Naito, M. and Hashimoto, Y.:
J. Am. Chem. Soc. 132, 5820-5826 (2010).
‣Structural development studies of anti-hepatitis C virus agents with a phenanthridinone skeleton.
Nakamura, M., Aoyama, A., Salim, M.T., Okamoto, M., Baba, M. Miyachi, H., Hashimoto, Y. and Aoyama H.:
Bioorg. Med. Chem. 18, 2402-2411 (2010).
‣LXXLL peptide mimetics as inhibitors of the interaction of vitamin D receptor with coactivators.
Mita, Y., Dodo, K., Noguchi-Yachide, T., Miyachi, H., Makishima, M., Hashimoto, Y. and Ishikawa, M.:
Bioorg. Med. Chem. Lett. 20, 1712-1717 (2010).
‣β-Naphthoflavone analogs as potent and soluble aryl hydrocarbon receptor agonists: improvement of solubility by disruption of molecular planarity.
Fujita, Y., Yonehara, M., Tetsuhashi, M., Noguchi-Yachide, T., Hashimoto Y. and Ishikawa, M.:
Bioorg. Med. Chem. 18, 1194-1203 (2010).
‣Identification of binding proteins of fusarielin A as actin and tubulin.
Noguchi-Yachide, T., Dodo, K., Aoyama, H., Fujimoto, H., Hori, M., Hashimoto, Y. and Kobayashi, H.:
Chem. Pharm. Bull. 58, 129-134 (2010).
2009
‣Lissoclibadins 814, polysulfur dopamine-derived alkaloids from the colonial ascidian Lissoclinum cf. badium.
Wang, W., Takahashi, O., Oda, T., Nakazawa, T., Ukai, K., Mangindaan, R.E., Rotinsulu, H., Wewengkang, D.S., Kobayashi, H., Tsukamoto, S. and Namikoshi, M.:
Tetrahedron 65, 9598-9603 (2009).
‣(25S)-Cholesten-26-oic acid derivatives from an Indonesian soft coral Minabea sp.
Wang, W., Lee, J.-S., Nakazawa, T., Ukai, K., Mangindaan, R.E., Wewengkang, D.S., Rotinsulu, H., Kobayashi, H., Tsukamoto, S. and Namikoshi, M.:
Steroids 74, 758-760 (2009).
‣Novel biphenylcarboxylic acid peroxisome proliferator-activated receptor (PPAR) δ selective antagonists.
Kasuga, J., Ishida, S., Yamasaki, D., Makishima, M., Doi, T., Hashimoto, Y. and Miyachi, H.:
Bioorg. Med. Chem. Lett. 19, 6595-6599 (2009).
‣Structure-activity relationship of bis-galloyl derivatives related to (-)-epigallocatechin gallete.
K. Dodo, T. Minato and Y. Hashimoto:
Chem. Pharm. Bull., 57(2): 190-194 (2009).
‣Polymethylated γ-carbolines with potent anti-bovine viral diarrhea virus (BVDV) activity.
H. Aoyama, K. Sako, S. Sato, M. Nakamura, H. Miyachi, Y. Goto, M. Okamoto, M. Baba and Y. Hashimoto
Heterocycles, 77(2):779-785 (2009).
‣Suppression of b-catenin signaling by liver X receptor ligands.
S. Uno, K. Endo, Y. Jeong, K. Kawana, H. Miyachi, Y. Hashimoto and M. Makishima:
Biochem. Pharmacol., 77(2): 186-195 (2009).
‣Dipheynylpentane skeleton as a multi-template for steroid skeleton-recognizing receptors/enzymes.
S. Hosoda, D. Matsuda, H. Tomoda and Y. Hashimoto:
Mini-Rev. Med. Chem., 9(5): 572-580 (2009).
‣Enhancement of chemically-induced HL-60 cell differentiation by 3,3'-diindolylmethane derivatives.
T. Noguchi-Yachide, M. Tetsuhashi, H. Aoyama and Y. Hashimoto:
Chem. Pharm. Bull., 57(5): 536-540 (2009).
‣ Induction of SREBP-1c mRNA by differentiation and LXR ligand in human keratinocytes.
A. Yokoyama, M. Makishima, M. Choi, Y. Cho, S. Nishida, Y. Hashimoto and T. Terui:
J. Invest. Dermatol., 129(6): 1395-1401 (2009).
‣Discovery of diphenylmethane analogs as anti-bovine viral diarrhea viral agents.
S. Hosoda, H. Aoyama, Y. Goto, M. T. A. Salim, M. Okamoto, M. Hashimoto, M. Baba and Y. Hashimoto:
Bioorg. Med. Chem. Lett., 19(12): 3157-3161 (2009).
‣PPARδ選択的アゴニストの創製と受容体-リガンド複合体構造情報を踏まえた選択性発現機構解明
春日淳一、大山拓次、中込泉、青山惇、迫久美子、槙島誠、広野修一、森川耿右、橋本祐一、宮地弘幸:
薬学雑誌, 129(6): 709-718 (2009).
‣Discovery of tetramethyltatrahydronaphthalene analogs as adult T-cell leukemia cells-selective proliferation inhibitors in a small chemical library constructed based on multi-template hypothesis.
M. Nakamura, T. Hamasaki, M. Tokitou, M. Baba, Y. Hashimoto, and H. Aoyama:
Bioorg. Med. Chem., 17(13): 4740-4746 (2009).
‣The peroxisome proliferator-activated receptor γ/retinoid X receptor α heterodimer targets the histone modification enzyme PR-Set7/Setd8 gene and regulates adipogenesis through a positive feedback loop.
K. Wakabayashi, M. Okamura, S. Tsutsumi , N. S. Nishikawa, T. Tanaka, I. Sakakibara, J. Kitakami, S. Ihara, Y. Hashimoto, T. Hamakubo, T. Kodama, H. Aburatani and J. Sakai:
Mol. Cell. Biol., 29(13): 3544-3555 (2009).
‣Application of a 3,3-diphenylpentane skeleon as a multi-template for creation of HMG-CoA reductase inhibitors.
S. Hosoda, D. Matsuda, H. Tomoda, M. Hashimoto, H. Aoyama and Y. Hashimoto:
Bioorg. Med. Chem. Lett., 19(15): 4228-4231 (2009).
‣Separation of α-glucosidase-inhibitory and liver X receptor-antagonistic activities of phenethylphenylphthalimide analogs and generation of LXRα-selective antagonists.
K. Motoshima, T. Noguchi-Yachide, K. Sugita, Y.Hashimoto and M. Ishikawa:
Bioorg. Med. Chem., 17(14): 5001-5014 (2009).
‣Adaptability and selectivity of human peroxisome proliferator-activated receptor (PPAR) pan agonists revealed from crystal structures.
T. Oyama, K. Toyota, T. Waku, Y. Hirakawa, N. Nagasawa, J. Kasuga, Y. Hashimoto, H. Miyachi and K. Morikawa:
Acta Crystallographica (D), D65(8): 786-795 (2009).
‣Liver X receptor (LXR) modulators with dibenz[b,f][1,4]oxazepin-11-one, (Z)-debenz[b,f]azocin- 6-one, and 11,12-dihydrodibenz[b,f]azocin-6-one skeleton.
A. Aoyama, H. Aoyama, M. Makishima, Y. Hashimoto and H. Miyachi:
Heterocycles, 78(9): 2209-2216 (2009).
‣Glycogen phosphorylase a inhibitors with a phenethylphenylphthalimide skeleton derived from thalidomide-related α-glucosidsase inhibitors and liver X receptor antagonists.
K. Motoshima, M. Ishikawa, K. Sugita and Y. Hashimoto:
Biol. Pharm. Bull., 32(9): 1618-1620 (2009).
‣Interaction of biological response modifier with proteins.
Y. Hashimoto:
Chapter 8 in “Protein Targeting with Small Molecules: Chemical Biology Techniques and Applications”, ed. by Hiroyuki Osada, p149-168, John Wiley & Sons, Inc., New Jersey, ISBN: 978-0-470-12053-8 (2009).
‣配座固定を基盤とした核内受容体LXRの新規リガンド創製
宮地弘幸、青山惇、橋本祐一:
MEDCHEM NEWS, 19(2): 30-37 (2009).
‣マルチテンプレート手法によるサリドマイドの構造展開と活性拡張.
橋本祐一:
和光純薬時報, 77(1): 2-5 (2009).
2008
‣Novel tubulin-polymerization inhibitor derived from thalidomide directly induces apoptosis in human multiple myeloma cells: Possible anti-myeloma mechanism of thalidomide.
T. Iguchi, T. Noguchi-Yachide, Y. Hashimoto, S. Nakazato, M. Sagawa, Y. Ikeda and M. Kizaki:
Int. J. Mol. Med., 21(1): 163-168 (2008).
‣Fusarieline A as an anti-angiogenic and antiproliferative agent: Basic biological characterization.
H. Fujimoto, H. Aoyama, T. Noguchi-Yachide, Y. Hashimoto and H. Kobayashi:
Chem. Pharm. Bull., 56(3): 298-304 (2008).
‣New tubulin-polymerization inhibitor derived from thalidomide: Implications for anti-myeloma therapy.
M. Kizaki and Y. Hashimoto:
Curr. Med. Chem., 15(8): 754-765 (2008).
‣γ-Carboline derivatives with anti-bovine viral diarrhea virus (BVDV) activity.
K. Sako, H. Aoyama, S. Sato, Y. Hashimoto and M. Baba:
Bioorg. Med. Chem., 16(7): 3780-3790 (2008).
‣Coordination of divalent metal cation to amide group to form adduct ion in FAB mass spectrometry: Implication of Zn2+ in enzymatic hydrolysis of amide bond.
H. Kobayashi, N. Morisaki, H. Miyachi and Y. Hashimoto:
Chem. Pharm. Bull., 56(5): 672-676 (2008).
‣Degradation-promoters of cellular inhibitor of apoptosis protein 1 based on bestatin and actinonin.
S. Sato, M. Tetsuhashi, K. Sekine, H. Miyachi, M. Naito, Y. Hashimoto and H. Aoyama:
Bioorg. Med. Chem., 16(8): 4685-4698 (2008).
‣Co-existence of α-glucosidase-inhibitory and liver X receptor-regulatory activities and their separation by structural development.
K. Dodo, A. Aoyama, T. Noguchi-Yachide, M. Makishima, H. Miyachi and Y. Hashimoto:
Bioorg. Med. Chem., 16(8): 4272-4285 (2008).
‣SAR-oriented discovery of peroxisome proliferator-activated receptor pan agonist with a 4-adamantylphenyl group as a hydrophobic tail.
Jun-ichi Kasuga, Daisuke Yamasaki, Kiyoshi Ogura, Motomu Shimizu, Mayumi Sato, M. Makishima, T. Doi, Y. Hashimoto and H. Miyachi:
Bioorg. Med. Chem. Lett., 18(3), 1110-1115 (2008).
‣Demonstration of direct binding of cIAP1 degradation-promoting bestatin analogs to BIR3 domain: Synthesis and application of fluorescent bestatin ester analogs.
S. Sato, H. Aoyama, H. Miyachi, M. Naito and Y. Hashimoto:
Bioorg. Med. Chem. Lett., 18(11), 3354-3358 (2008).
‣Progesterone receptor antagonists with a 3-phenylquinazoline-2,4-dione/2-phenyl -isoquinoline-1,3-dione skeleton.
A. Nakagawa, S. Uno, M.Makishima, H. Miyachi and Y. Hashimoto:
Bioorg. Med. Chem., 16(14), 7046-7054 (2008).
‣4-(Anilino)pyrrole-2-carboxamides: Novel non –steroidal/non-anilide type androgen antagonists effecrive upon human prostate tumor LNCaP cells with mutated nuclear androgen receptor.
K. Wakabayashi, K. Imai, H. Miyachi, Y. Hashimoto and A. Tanatani:
Bioorg. Med. Chem., 16(14), 6799-6812 (2008).
‣Improvement of the transactivation activity of phenylpropanoic acid-type peroxisome proliferator-activated receptor pan agonists: Effect of introduction of fluorine at the linker part.
Kasuga J, Oyama T, Hirakawa Y, Makishima M, Morikawa K, Hashimoto Y, Miyachi H:
Bioorg Med Chem Lett. 18(16), 4525-4528 (2008).
‣Structural Development Studies of Subtype-Selective Ligands for Peroxisome Proliferator-Activated Receptors (PPARs) Based on the 3,4-Disubstituted Phenylpropanoic Acid Scaffold as a Versatile Template.
Miyachi H, Hashimoto Y:
PPAR Res. 2008;2008:689859. PMID: 18566690
‣1alpha,25-Dihydroxyvitamin D(3)-26,23-lactam analogues function as vitamin D receptor antagonists in human and rodent cells
Ishizuka S, Kurihara N, Hiruma Y, Miura D, Namekawa J, Tamura A, Kato-Nakamura Y, Nakano Y, Takenouchi K, Hashimoto Y, Nagasawa K, Roodman GD:
J Steroid Biochem Mol Biol. Jun;110(3-5):269-77 (2008).
‣Antiproliferative and apoptosis-inducing activities of alkyl gallate and gallamide derivatives related to (-)-epigallocatechin gallete.
K. Dodo, T. Minato, T. Noguchi-Yachide, M. Suganuma and Y. Hashimoto:
Bioorg. Med. Chem., 16(17), 7975-7982 (2008).
‣LXR antagonists with a 5-substituted phenanthridin-6-one skeleton: Synthesis and LXR transrepression activities of conformationally restricted carba-T0901317 analogs.
A. Aoyama, H. Aoyama, K. Soso, M. Makashima, Y. Hashimoto and H. Miyachi:
Heterocycles. 76 (1), 137-142 (2008).
‣Structural development of benzhydrol-type 1’-acetoxychavicol acetate(ACA) analogs as human leuchemia cell-growth inhibitors based on quantitative structure-activity relationship (QSAR) analysis.
T. Misawa, H. Aoyama, T. Furuyama, K. Dodo, M. Sagawa, H. Miyachi, M. Kizaki and Y. Hashimoto:
Chem. Pharm. Bull., 56(10): 1490-1495 (2008).
‣Thalidomide as a multi-template for development of biologically active compounds.
Y. Hashimoto:
Arch. Pharm. Chem. Life Sci. 341,536-547 (2008).
‣Thiourea-catalyzed Morita-Baylis-Hilman Reaction.
Y. Sohtome, N. Takemura, R. Takagi, Y. Hashimoto and K. Nagasawa:
Tetrahedron, 64(40): 9423-9429 (2008).
‣Peroxisome proliferators-activated receptor (PPAR) agonists with 3,4-dihydro-2H- benzo[e][1,3]oxazine and 2,3,4,5-tetrahydrobenzo[f][1,4]oxazepine skeletons: Effects of cyclization of linker moiety on PPAR-agonistic activity.
K. Ohgane, J. Kasuga, T. Ohyama, Y. Hirakawa, K. Morikawa, M. Makishima, Y. Hashimoto and H. Miyachi:
Heterocycles, 75(9): 2187-2192 (2008).
‣Development of bifunctional acyclic hydroxyl-guanidine organocatalyst: Application to asymmetric nucleophilic epoxidation.
B. Shin, S. Tanaka, T. Kita, Y. Hashimoto and K. Nagasawa:
Heterocycles, 76(1): 801-810 (2008).
‣Structure-based design and synthesis of fluorescent PPAR a/d co-agonist and its application as a probe for fluorescent polarization assay of PPARd ligands.
Y. Araya, J. Kasuga, K. Toyota, Y. Hirakawa, T. Oyama, M. Makishima, K. Morikawa, Y. Hashimoto and H. Miyachi:
Chem. Pharm. Bull., 56(9): 1357-1359 (2008).
‣X-Ray crystallographic identification of bisulfite-uracil adduct as sodium 5,6-dihydrouracil 6-sulfonate.
M. Kaneda, Y. Hashimoto and H. Hayatsu:
Nucleic Acids Symp. Ser., 52(1): 451-452 (2008).
2007
‣Origin of chemoselectivity of TMP zincate bases and differences between TMP zincate and alkyl lithium reagents: A DFT study on model systems
M. Uchiyama, Y. Matsumoto, S. Usui, Y. Hashimoto and K. Morokuma
Angew. Chem. Int. Ed. 2007, 46(6), 926-929.
‣Hydrolyzed Metabolites of Thalidomide: Synthesis and TNF-α Production-Inhibitory Activity
T. Nakamura, T. Noguchi, H. Miyachi and Y. Hashimoto
Chem. Pharm. Bull., 2007, 55(4), 651-654.
‣Theoretical Studies on ortho-Oxidation of Phenols with Dioxygen Mediated by Dicopper Complex: Hints for a Catalyst with the Phenolase Activity of Tyrosinase
H. Naka, Y. Kondo, S. Usui, Y. Hashimoto, M. Uchiyama
Adv. synth. Catal., 2007, 349(4-5), 595-600.
‣Structural development studies of nuclear receptor ligands
S. Hosoda and Y. Hashimoto
Pure Appl. Chem., 2007, 79(4), 615-626.
‣Development of Tubulin-Polymerization Inhibitors Based on the Thalidomide Skeleton
H. Aoyama, T. Noguchi, T. Misawa, T. Nakamura, H. Miyachi, Y. Hashimoto and H. Kobayashi
Chem. Pharm. Bull., 2007, 55(6), 944-949.
‣Liver X receptor antagonists with a phthalimide skeleton derived from thalidomide-related glucosidase inhibitors
T. Noguchi-Yachide, A. Aoyama, M. Makishima, H. Miyachi and Y. Hashimoto
Bioorg. Med. Chem. Lett., 2007, 17(14), 3957-3961.
‣Design, synthesis, and evaluation of potent, structurally novel peroxisome proliferator-activated receptor (PPAR) δ-selective agonists
J. Kasuga, I. Nakagome, A. Aoyama, K. Sako, M. Ishizawa, M. Ogura, M. Makishima, S. Hirono, Y. Hashimoto and H. Miyachi
Bioorg. Med. Chem., 2007, 15(15), 5177-5190.
‣Design, synthesis, and evaluation of isoindolinone-hydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors
S. Lee, C. Shinji, K. Ogura, M. Shimizu, S. Maeda, M. Sato, M. Yoshida, Y. Hashimoto and H. Miyachi
Bioorg. Med. Chem. Lett., 2007, 17(17), 4895-4900.
‣3,3-Diphenylpentane skeleton as a steroid skeleton substitute: Novel inhibitors of human 5α-reductase 1
S. Hosoda and Y. Hashimoto
Bioorg. Med. Chem. Lett., 2007, 17(19), 5414-5418.
‣Structural development of liver X receptor (LXR) antagonists derived from thalidomide-related glucosidase inhibitors
T. Noguchi-Yachide, H. Miyachi, H. Aoyama, A. Aoyama, M. Makishima and Y. Hashimoto
Chem. Pharm. Bull., 2007, 55(12), 1750-1754.
‣Nucleophilic asymmetric epoxidation catalyzed by cyclic guanidines
T. Kita, B. Shin, Y. Hashimoto and K. Nagasawa
Heterocycles, 2007, 73, 241-247.
‣Direct ortho cupration: A new route to regioselectively functionalized aromatics
S. Usui, Y. Hashimoto, J. V. Morey, A. E. H. Wheatley and M. Uchiyama
J. Am. Chem. Soc., 2007, 129(49), 15102-15103.
‣Design, synthesis, and evalution of non-steroidal farnesoid X receptor (FXR) antagonist
M. Kainuma, M. Makishima, Y. Hashimoto, and H. Miyachi
Bioorg. Med. Chem., 2007, 15(7), 2587-2600.
‣Synthesis and biological activities of batzelladine derivatives
J. Shimokawa, Y. Iijima, Y. Hashimoto, H. Chiba, H. Tanaka and K. Nagasawa
Heterocycles, 2007, 72, 145-150.
‣Design, synthesis, and evaluation of characteristic subtype-selective peroxisome proliferator-activated receptor (PPAR) ligands
Miyachi H.
Current Med. Chem., 2007, 14(22), 2335-2343.
‣大学における科学活動としての医薬化学:ドラマタイプ手法とマルチテンプレート手法の発信
橋本祐一
MEDCHEM NEWS, 2007, 17(1), 20-23.
‣大学院講義有機化学演習編( 生物有機化学)
橋本祐一
大学院講義有機化学演習編, (野依良治・柴崎正勝・鈴木啓介・玉夫皓平・中筋一弘・奈良坂紘一 編)、東京化学同人、東京、pp75-80, pp170-176,2007, 17(1), 20-23.
‣核内レセプターリガンドの創製研究
宮地弘幸,橋本祐一
化学フロンディァ⑲創薬をめざす有機合成戦略 --- 進化する医薬品づくり, (宍戸宏造・新藤充 編)、化学同人,京都、p149-155 (2007).
‣創薬研究の基礎知識---標的となる生体分子
橋本祐一
ベーシック薬学教科書シリーズ6「創薬科学・医薬化学」, (橘高敦史 編)、化学同人、京都、第6章, p95-131 (2007).
‣代表的な医薬品---気管支喘息治療薬、消化性潰瘍薬、糖尿病治療薬"
橋本祐一
ベーシック薬学教科書シリーズ6「創薬科学・医薬化学」, (橘高敦史 編)、化学同人、京都、第11-13章, p217-248 (2007).
2006
‣Design and synthesis of substitited phenylpropanoic acid derivatives as human peroxisome proliferator activated receptor α/δ dual agonists
J. Kasuga, M. Makishima, Y. Hashimoto and H. Miyachi
Bioorg. Med. Chem. Lett. 2006, 16(3), 554-558
‣Concise and efficient asymmetric synthesis of (S)-2-ethylphenylpropanoic acid derevatives: Dual agonists for human peroxisome proliferator activated receptor α and δ
J. Kasuga, Y. Hashimoto and H. Miyachi
Bioorg. Med. Chem. Lett. 2006, 16(4), 771-774
‣Practical synthesis and evaluation of the biological activities of 1α,25-dihydroxyvitamin D3 antagonists, 1α,25-dihydroxyvitamin D3-26,23-lactams. Designed on the basis of the helix 12-folding inhibition hypothesis
Y. Nakano, Y. Kato, K. Imai, E. Ochiai, J. Namekawa, S. Ishizuka, K. Takenouchi, A. Tanatani, Y. Hashimoto and K. Nagasawa
J. Med. Chem. 2006, 49(8), 2398-2406
‣Anti-angiogenic activity of basic-type, selective cyclooxygenase (COX)-1 inhibitors
H. Sano, T. Noguchi, A. Miyajima, Y. Hashimoto and H. Miyachi
Bioorg. Med. Chem. Lett. 2006, 16(11), 3068-3072
‣Diphenylmethane skeleton as a multi-template for nuclear receptor ligands: Preparation of FXR and PPAR ligands
M. Kainuma, J. Kasuga, S. Hosoda, K. Wakabayashi, A. Tanatani, K. Nagasawa, H. Miyachi, M. Makishima and Y. Hashimoto
Bioorg. Med. Chem. Lett. 2006, 16(12), 3213-3218
‣Effects of immunomodulatory derivatives of thalidomide (IMiDs) and their analogs on cell-differentiation, cyclooxygenase activity and angiogenesis
H. Fujimoto, T. Noguchi, H. Kobayashi, H. Miyachi and Y. Hashimoto
Chem. Pharm. Bull. 2006, 54(6), 855-860
‣Ligands with a 3,3-diphenylpentane skeleton for nuclear vitamin D and androgen receptors: Dual activities and metabolic activation
S. Hosoda, A. Tanatani, K. Wakabayashi, M. Makishima, K. Imai, H. Miyachi, K. Nagasawa and Y. Hashimoto
Bioorg. Med. Chem. 2006, 14(16), 5489-5502
‣Tubulin polymerization inhibitors with a fluorinated phthalimide skeleton derived from thalidomide
T. Yanagawa, T. Noguchi, H. Miyachi, H. Kobayashi and Y. Hashimoto
Bioorg. Med. Chem. Lett. 2006, 16(18), 4748-4751
‣Mono- and dihydroxylated metabolites of thalidomide: synthesis and TNF-α production-inhibitory activity
T. Nakamura, T. Noguchi, H. Kobayashi, H. Miyachi and Y. Hashimoto
Chem. Pharm. Bull. 2006, 54(12), 1709-1714
‣Design, synthesis, and evaluation of a novel series of α-substituted phenylpropanoic acid derivatives as human peroxisome proliferator-activated receptor (PPAR) α/δ dual agonists for the treatment of metabolic syndrome
J. Kasuga, D. Yamasaki, Y. Araya, A. Nakagawa, M. Makishima, T. Doi, Y. Hashimoto and H. Miyachi
Bioorg. Med. Chem. 2006, 14(24), 8405-8414
‣Crystal structure of Vigna radiata cytokinin-specific binding protein in complex with zeatin
O. Pasternak, G. D. Bujacz, Y. Fujimoto, Y. Hashimoto, F. Jelen, J. Otlewski, M. M. Sikorski and M. Jaskolski
The Plant Cell 2006, 18, 2622-2634
‣Design, synthesis, and evaluation of cyclic amide/imide-bearing hydroxamic acid derivatives as class-selective histone deacetylase (HDAC) inhibitors
C. Shinji, S. Maeda, K. Imai, M. Yoshida, Y. Hashimoto and H. Miyachi
Bioorg. Med. Chem. 2006, 14(22), 7625-7651
‣Transgenic rescue of erythroid 5-aminolevulinate synthase-deficient mice results in the formation of ring sideroblasts and siderocytes
O. Nakajima, S. Okano, H. Harada, T. Kusaka, X. Gao, T. Hosoya, N. Suzuki, S. Takahashi and M. Yamamoto
Genes Cells 2006, 11, 685-700
‣Diastereoselective Henry reaction catalyzed by guanidine-thiourea bifunctional organocatalyst
Y. Sohtome, N. Takemura, T. Iguchi, Y. Hashimoto and K. Nagasawa
Synlett 2006, 1, 144-146
‣Diastereoselective and Enantioselective Henry (Nitroaldol) Reaction Utilizing a Guanidine-Thiourea Bifunctional Organocatalyst
Y. Sohtome, Y. Hashimoto and K. Nagasawa
Eur. J. Org. Chem. 2006, 13, 2894-2897
‣Recent progress of the medicinal chemistry research on peroxisome proliferator-activated receptor for the treatment of metabolic syndrome
H. Miyachi
Current Bioactive Compound 2006, 2, 151-159
‣糖尿病の薬物療法 (分担執筆)
宮地 弘幸
PPARをターゲットとした創薬 (編者: 難波光義、谷澤幸生) 2006, 226-229, 文光堂
2005
‣Tubulin-polymerization inhibitors derived from thalidomide
S. Inatsuki, T. Noguchi, H. Miyachi, S. Oda, T. Iguchi, M. Kizaki, Y. Hashimoto, and H. Kobayashi
Bioorg. Med. Chem. Lett., 2005, 15, 321-325.
‣Enhancement of all-trans retinoic acid-induced HL-60 cell differentiation by thalidomide and its metabolites
T. Noguchi, C. Shinji, H. Kobayashi, M. Makishima, H. Miyachi, and Y. Hashimoto
Biol. Pharm. Bull., 2005, 28, 563-564
‣Novel non-steroidal/non-anilide type androgen antagonists: discovery of 4-substituted pyrrole-2-carboxamides as a new scaffold for androgen receptor ligands
K. Wakabayashi, H. Miyachi, Y. Hashimoto and A. Tanatani
Bioorg. Med. Chem., 2005, 13(8), 2837-2846
‣Design and synthesis of subtype-selective cyclooxyganase (COX) inhibitors derived from thalidomide
H. Sano, T. Noguchi, A. Tanatani, Y. Hashimoto and H. Miyachi
Bioorg. Med. Chem., 2005, 13(9), 3079-3091
‣Helical Structure of N-Alkylated Poly(p-benzamide)s
A. Tanatani, A. Yokoyama, I. Azumaya, Y. Takakura, C. Mitsui, M. Shiro, M. Uchiyama, A. Muranaka, N. Kobayashi, T. Yokozawa
J. Am. Chem. Soc., 2005, 127, 8553-8561
‣A new class of androgen receptor antagonists bearing carborane in place of a steroidal skeleton
S. Fujii, Y. Hashimoto, T. Suzuki, S. Ohta and Y. Endo
Bioorg. Med. Chem. Lett., 2005, 15, 227-230
‣Cell Differentiation Inducers Derived from Thalidomide
T. Noguchi, H. Miyachi, R. Katayama, M. Naito, and Y. Hashimoto
Bioorg. Med. Chem. Lett., 2005, 15, 3212-3215
‣Potent Androgen Antagonists Based on Carborane as a Hydropobic Core Structure
S. Fujii, T. Goto, K. Ohta, Y. Hashimoto, T. Suzuki, S. Ohta and Y. Endo
J. Med. Chem., 2005, 48, 4654-4662
‣Nuclear receptor antagonists designed based on the helix-folding inhibition hypothesis
Y. Hashimoto, H. Miyachi
Bioorg. Med. Chem., 2005, 13(17), 5080-5093
‣Ligands with dual vitamin D3-agonistic and androgen-antagonistic activities
S. Hosoda, A. Tanatani, K. Wakabayashi, Y. Nakano, H. Miyachi, K. Nagasawa and Y. Hashimoto
Bioorg. Med. Chem. Lett., 2005, 15, 4327-4331
‣Design and synthesis of phthalimide-type histone deacetylase inhibitors
C. Shinji, T. Nakamura, S. Maeda, M. Yoshida, Y. Hashimoto and H. Miyachi
Bioorg. Med. Chem. Lett., 2005, 15, 4427-4431
‣Angiogenesis inhibitors derived from thalidomide
T. Noguchi, H. Fujimoto, H. Sano, A. Miyajima, H. Miyachi and Y. Hashimoto
Bioorg. Med. Chem. Lett., 2005, 15(24), 5509-5513
‣Guanidine-thiourea bifunctional organocatalyst for the asymmetric Henry (nitroaldol) reaction
Y. Sohtome, Y. Hashimoto and K. Nagasawa
Adv. Synth. Catal., 2005, 347, 1643-1648
‣Total synthesis of (+)-batzelladine A and (-)-batzelladine D, and identification of their target protein
J. Shimokawa, T. Ishiwata, K. Shirai, H. Koshino, A. Tanatani, T. Nakata, Y.Hashimoto and K. Nagasawa
Chem. Eur. J., 2005, 11, 6878-6888
‣Analysis of patent applications relating to peroxisome proliferator-activated receptor (PPAR) ligands in 2004
H. Miyachi
Expert Opin. Ther. Patent., 2005, 15, 1521-1530
‣Lissoclibadins 1-3, three new polysulfur alkaloids, from the ascidian Lissoclinum cf. badium
HW Liu, T. Fujiwara, T. Nishikawa, Y. Mishima, H. Nagai, T. Shida, K. Tachibana, H. Kobayashi, REP. Mangindaan and M. Namikoshi
Tetrahedron, 2005, 61(36), 8611-8615
‣Seven new meroditerpenoids, from the marine sponge Strongylophora strongylata, that inhibited the maturation of starfish oocytes
HW. Liu, M. Namikoshi, K. Akano, H. Kobayashi, H. Nagai and XS. Yao
J. Asian Nat. Prod. Res., 2005, 7(4), 661-670
‣サリドマイドとがん治療
野口友美,橋本祐一
がん分子標的治療, 2005, 3, 16-23
‣薬害の克服を目指した創薬化学 サリドマイドをマルチ創薬テンプレートとして活用したサリドマイドの構造展開と活性拡張
宮地弘幸,橋本祐一
ファルマシア, 2005, 41, 33-37
‣PPARを標的とした創薬
影近弘之,宮地弘幸
日本臨床, 2005, 63, 549-555
‣新たなる創薬手法によるサリドマイドの構造展開とがん治療
橋本祐一
血液・腫瘍科, 2005, 51(1), 7-15
‣レチノイド受容体
橋本祐一
生物薬科学実験講座 Vol.7-1. 情報伝達物質[1] 受容体, 石橋貞彦・市川厚・堅田利明編集、廣川書店、 pp. 218-230、2005
‣生体内分子と反応する医薬品
橋本祐一
スタンダード薬学シリーズ 第3巻 化学系薬学.ターゲット分子の合成と生体分子・医薬品の化学 第15章 日本薬学会編、東京化学同人、 pp. 235-240、2005
‣レチノイドとサリドマイドをリードとする生物応答調節剤の創製研究 — 構造展開と活性拡張—
ケミカルバイオロジー・ケミカルゲノミクス 半田宏編、シュプリンガー・フェアラーク東京、 pp. 135-146、2005
‣立体化学のための分析技術: NMR による解析
小林久芳、降旗一夫
ぶんせき、2005, 3, 118-124
2004
‣Development of novel chiral urea catalysts for the hetero-Michael reaction
Y. Sohtome, A. Tanatani, Y. Hashimoto, and K. Nagasawa
Chem. Pharm. Bull., 52(4), 477-480, 2004
‣Thalidomide as a nitric oxide synthase inhibitor and its structural development
R. Shimazawa, H. Sano, A. Tanatani, H. Miyachi, and Y. Hashimoto
Chem. Pharm. Bull., 52(4), 498-499, 2004
‣Enantioselective total synthesis of batzelladine A
J. Shimokawa, K. Shirai, A. Tanatani, Y. Hashimoto, K. Nagasawa
Angew. Chem. Int. Ed., 43(12), 1559-62, 2004
‣Thalidomide as a multitarget drug and its application as a template for drug design
Y. Hashimoto, A. Tanatani, K. Nagasawa, and H. Miyachi
Drugs of the Future, 29(4), 383-391, 2004
‣Synthesis of 1α,25-dihydroxyvitamin D3-26,23-lactams (DLAMs), a novel series of 1α,25-dihydroxyvitamin D3 antagonist
Y. Kato, Y. Nakano, H. Sano, A. Tanatani, H. Kobayashi, R. Shimazawa, H. Koshino, Y. Hashimoto, and K. Nagasawa
Bioorg. Med. Chem. Lett., 14(10), 2579-2583, 2004
‣Evaluation of series of isobenzofuranone dimers as PKCα ligands: implication for the distance between the two ligand binding sites
Y. Baba, S. Mayumi, G. Hirai, H. Kawasaki, Y. Ogoshi, T. Yanagisawa, Y. Hashimoto, and M. Sodeoka
Bioorg. Med. Chem. Lett., 14(11), 2969-2972, 2004
‣Synthetic ligands for peroxisome proliferator-activated receptor-α, review of the patent literature 2000-2003
H. Miyachi
Expert Opin. Ther. Patents, 14(5), 607-618, 2004
‣N-Phenylphthalimide-type cyclooxygenase (COX) inhibitors derived from thalidomide: Substituent effects on subtype selectivity
H. Sano, T. Noguchi, A. Tanatani, H. Miyachi, and Y. Hashimoto
Chem. Pharm. Bull., 52(8), 1021-1022, 2004
‣Development of bis-thiourea-type organocatalyst for asymmetric Baylis-Hillman reaction
Y. Sohtome, A. Tanatani, Y. Hashimoto, and K. Nagasawa
Tetrahedron Lett., 45, 5589-5592, 2004
‣Phenylhomophthalimide-type NOS inhibitors derived from thalidomide
T. Noguchi, H. Sano, R. Shimazawa, A. Tanatani, H. Miyachi, and Y. Hashimoto
Bioorg. Med. Chem. Lett., 14(16), 4141-4145, 2004
‣Recent progress in research on peroxisome proliferator-activated receptor α-selective ligands
H. Miyachi
IDrugs, 7(8), 746-754, 2004
‣The use of PPARα/γ dual agonists for the treatment of metabolic syndromes
H. Miyachi
Expert Opin. Ther. Patents, 14(12), 1797-1801, 2004
‣サブタイプ及び種選択的ペルオキシゾーム増殖剤応答性受容体(PPAR)αリガンドの創製
宮地弘幸
YAKUGAKU ZASSHI, 124(11) 803-813, 2004
2003
‣Fluorescent bioprobes for visualization of puromycin-sensitive aminopeptidase in living cell
H. Kakuta, Y. Koiso, K. Nagasawa and Y. Hashimoto
Bioorg. Med. Chem. Letters, 13, 83-86, 2003
‣Absolute structure, biosynthesis, and anti-microtubule activity of phomopsidin, isolated from a marine-derived fungus Phomopsis sp.
H. Kobayashi, S. Meguro, T. Yoshimoto and M. Namikoshi
Tetrahedron, 59, 455-459, 2003
‣Structural development of synthetic retinoids and thalidomide-related molecules
Y. Hashimoto
Cancer Chemother. Pharmacol., 52(Suppl 1), S16-S23, 2003
‣Anti-androgens with full antagonistic activity toward human prostate tumor LNCaP cells with mutated androgen receptor
T. Ishioka, A. Tanatani, K. Nagasawa and Y. Hashimoto
Bioorg. Med. Chem. Letters, 13, 2655-2658, 2003
‣Novel heteroatom-containing vitamin D3 analogs: Efficient synthesis of 1α,25-dihydroxyvitamin D3-26,23-lactam
Y. Kato, Y. Hashimoto and K. Nagasawa
Molecules, 8, 488-499, 2003
‣Cyclooxygenase inhibitors derived from thalidomide
M. Suizu, Y. Muroya, H. Kakuta, H. Kagechika, A. Tanatani, K. Nagasawa and Y. Hashimoto
Chem. Pharm. Bull., 51(9), 1098-1102, 2003
‣Synthesis of marine guanidine alkaloids and their application as chemical/biological tools
K. Nagasawa and Y. Hashimoto
Chem. Record, 3 201-211, 2003
‣Specific nonpeptide inhibitors of puromycin-sensitive aminopeptidase with a 2,4(1H,3H)-quinazolinedione skeleton
H. Kakuta, A. Tanatani, K. Nagasawa and Y. Hashimoto
Chem. Pharm. Bull., 51(11), 1273-1282, 2003
‣Conversion of Ca2+ salt of an organic compound to its Li+ salt to simplify the fast atom bombardment mass spectrum
N. Morisaki, H. Kobayashi, K. Nagasawa, Y. Baba, M. Sodeoka and Y. Hashimoto
Chem. Pharm. Bull., 51(11), 1341-1344, 2003
‣Stereoselective synthesis of novel ptilomycalin A analogs via successive 1,3-dipolar cycloaddition reactions and their Ca2+-ATPase inhibitory activity
A. Georgieva, M. Hirai, Y. Hashimoto, T. Nakata, Y. Ohizumi, K. Nagasawa
Synthesis, 1427-1432, 2003
‣Transcriptional regulation of cytosol and membrane alanyl-aminopeptidase in human T cell subsets
A. Bukowska, J. Tadje, M. Arndt, C. Wolke, T. Kähne, J. Bartsch, J. Faust. K. Neubert, Y. Hashimoto, and U. Lendeckel
Biol. Chem., 384(4) 657-665, 2003
‣サリドマイドの過去・現在・未来
橋本祐一
ファルマシア, 39(4), 315-319, 2003
‣癌にきく? 使用広がるサリドマイド
橋本祐一
Medical Technology, 31(6), 571-572, 2003
‣特集:サリドマイドの最近の話題と展望 1. サリドマイドの薬理作用とその構造展開
橋本祐一
血液フロンティア, 13(7), 11(883)-21(893), 2003
‣サリドマイドの構造展開と活性拡張
長澤和夫,橋本祐一
細胞工学, 22(2), 152-155, 2003
‣サリドマイドの新しい適応
橋本祐一
現代医療, 35(7), 1615-1619, 2003
2002
‣Conformation of ligands bound to the muscarinic acetylcholin receptor.
H. Furukawa, T. Hamada, M. K. Hayashi, T. Haga, H. Hirota, S. Yokoyama, K. Nagasawa, M. Ishiguro
Mol. Pharmacol., 62, 778-787, 2002.
‣Novel non-steroidal/non-anilide type androgen antagonists with isoxazolone moiety.
T. Ishioka, A. Kubo, Y. Koiso, K. Nagasawa, A. Itai, Y. Hashimoto
Bioorg. Med. Chem., 10, 1555-1566, 2002.
‣Thalidomide and its analogues as cyclooxygenase inhibitors.
T. Noguchi, R. Shimazawa, K. Nagasawa, Y. Hashimoto
Bioorg. Med. Chem. Lett., 12, 1043-1046, 2002.
‣Total synthesis of crambescidine 359.
K. Nagasawa, A. Georgieva, H. Koshino, T. Nakata, T. Kita, Y. Hashimoto
Org. Lett., 4, 177-180, 2002.
‣Novel mannich-type nucleophilic substitution reaction with tertiary aromatic amines.
H. Takahashi, N. Kashiwa, Y. Hashimoto, K. Nagasawa
Tetrahedron Lett., 43, 2935-2938, 2002.
‣Coordination of sodium cation to an oxygen function and olefinic double bond to form molecular adduct ion in fast atom bombardment mass spectrometry.
N. Morisaki, H. Kobayashi, Y. Yamamura, M. Morisaki, K. Nagasawa, Y. Hashimoto
Chem. Pharm. Bull., 50, 935-940, 2002.
‣Nuclephilic substitution on 4-hydroxymethylanilines under neutral conditions via aza quinone methide intermediate.
H. Takahashi, N. Kashiwa, H. Kobayashi, Y. Hashimoto, K. Nagasawa
Tetrahedron Lett., 43, 5751-5753, 2002.
‣C2-symmetric chiral pentacyclic guanidine: A novel phase-transfer catalyst for the asymmetric alkylation of tert-butyl glycinate schiff base.
T. Kita, A. Georgieva, Y. Hashimoto, T. Nakata, K. Nagasawa
Angew. Chem., Int. Ed., 41, 2832-2834, 2002.
‣Novel retinoid X receptor antagonists: Specific inhibition of retinoid synergism in RXR-RAR heterodimer actions.
B. Takahashi, K. Ohta, E. Kawachi, H. Fukasawa, Y. Hashimoto, H. Kagechika
J. Med. Chem., 45, 3227-3330, 2002.
‣Synthesis and mechanism of action of novel pyrimidinyl pyrazole derivatives possessing antiproliferative activity.
H. Ohki, K. Hirotani, H. Naito, S. Ohsuki, M. Minami, A. Ejima, Y. Koiso Y. Hashimoto
Bioorg. Med. Chem. Lett., 12, 3191-3193, 2002.
‣Stereoselective synthesis of tricyclic guanidine, the key component of the batzelladine alkaloids.
K. Nagasawa, T. Ishiwata, Y. Hashimoto, T. Nakata
Tetrahedron Lett., 43, 6383-6385, 2002.
‣Total synthesis of batzelladien D.
T. Ishiwata, T. Hino, H. Koshino, Y. Hashimoto, T. Nakata, K. Nagasawa
Org. Lett., 4, 2921-2924, 2002.
‣Synthesis of novel heteroatom-containing Vitamin D3 Analogs.
Y. Kato, K. Nagasawa, Y. Koiso, H. Kobayashi, Y. Hashimoto
Vitamin, 76, 151, 2002.
‣A new screening method for antimitotic substances and isolation of glycolipids as stimulators of tubulin polymerization from Okinawa sponge pseudoceratina sp..
S. Meguro, M. Namikoshi, H. Kobayashi
J. Antibiot., 55, 256-262, 2002.
‣Inhibitors of microtubule assembly produced by the marine fungus strain TUF 98F139 collected in Palau.
M. Namikoshi, S. Suzuki, S. Meguro, H. Kobayashi, Y. Mine, I. Kasuga
J. Tokyo Univ. Fish., 88, 1-6, 2002.
‣Distribution of marine filamentous fungi associated with marine sponges in Coral Reefs of Palau and Bunaken Island, Indonesia.
M. Namikoshi, K. Akano, H. Kobayashi, Y. Koike, A. Kitazawa, A. B. Rondonuwu, S. Prarasik
J. Tokyo Univ. Fish., 88, 15-20, 2002.
‣サリドマイド事件は防げたか --- 光学活性と催奇形性 ---
橋本祐一
現代化学, No. 370, p64-65, 2002年, 1月号.
‣Structural development of biological response modifiers based on thalidomide.
Y. Hashimoto
Bioorg. Med. Chem., 10, 461-479, 2002.
‣サリドマイドのマルチ創薬テンプレートとしての活用---ドラマタイプ創薬の1例.
橋本祐一
Bioベンチャー, 2, 43-49, 2002.
‣Structural development of biological response modifiers based on retinoids and thalidomide.
Y. Hashimoto
Mini-Rev. Med. Chem., 2, 543-551, 2002.
2001
‣Asymmetric synthesis of a 3-acyltetronic acid derivative,RK-682,and formation of its calcium salt during silica gel colimn chromatography
M. Sodeoka, R. Sampe, S. Kojima, Y. Baba, N. Morisaki, and Y. Hashimoto
Chem. Pharm. Bull., 49, 206-212, (2001)
‣Specific inhibitor of puromycin-sensitive aminopeptidase with a homophthalimide skeleton: Identification of the target molecule and a structure-activity relationship study
M. Komoda, H. Kakuta, H. Takahashi, Y. Fujimoto, S. Kadoya, F. Kato, and Y. Hashomoto
Biol. Med. Chem., 9, 121-131, (2001)
‣Glycosylative inactivation of chalcomycin and tylosin by a clinically isolated Nocardia asteroides strain
N. Morisaki, Y. Hashimoto, K. Furihata, K. Yazawa, M. Tamura and Y. Mikami
J. Antibiotics, 54, 157-165, (2001)
‣Formaldehyde-mediated Modification of natural deoxyguanosine with amines: One-pot cyclization as a molecular model for genotoxicity
H. Takahashi, and Y. Hashimoto
Bioorg. Med. Chem. Lett., 729-731, 11, (2001)
‣α-Glucosidase inhibitors with a 4,5,6,7-tetrachlorophthalimide skeleton pendanted with a cycloalkyl or dicarba-cloro-dodecaborane group
S. Sou, H. Takahashi, R. Yamasaki, H. Kagechika, Y. Endo, and Y. Hashimoto
Chem. Pharm. Bull., 49, 791-793, (2001)
‣Thymidine phosphorylase inhibitors with a homophthalimide skelaton
T. Kita, H.Takahashi, and Y. Hashimoto
Biol. Pharm. Bull., 24, 860-862, (2001)
‣Aminopeptidase inhibitors: 3-(2,6-diethylphenyl)-2,4(1H,3H) quinazolinedione and N-(2,6-diethylphenyl)-2-amino-4H-3,1-benzoxazin-4-one
H. Kakuta, Y. Koiso, H. Takahashi, K. Nagasawa, and Y. Hashimoto
Heterocycles, 55, 1433-1438, (2001)
‣A new macrocyclic trichothecene, 12, 13-deoxyroridin E, produced by the marine-derived fungus Myrothecium roridum collected in Palau
M. Namikoshi, K. Akano, S. Meguro, I. Kasuga, Y. Mine, T. Takahashi and H. Kobayashi
J. Nat. Prod., 64, 396-398, (2001)
‣Novel formaldehyde-mediated dimerization reaction of N-alkyl-1-naphthylamine derivatives under mild/neutral conditions; Application to synthesis of naphthylamine-derived macrocycles
H. Takahashi, Y. Hashimoto, and K. Nagasawa
Heterocycles, 55, 2305-2313, (2001)
‣Enzyme inhibitors derived from thalidomide
H. Kakuta, H. Takahashi, S. Sou, T. Kita, K. Nagasawa and Y. Hashimoto
Recent Res. Devel. Medicinal Chem., 1, 189-211, (2001)
2000
‣ヒト白血病細胞K562細胞の細胞分化における化学制御
小磯邦子,中島修,松村大輔,藤本康之,橋本祐一
薬学雑誌, 120, 104-112, (2000)
‣Cleavage and inactivation of antiapoptotic Akt/PBK by caspases during apoptosis
S. Rokudai, N. Fujita, Y. Hashimoto, and T. Tsuruo
J. Cell. Physiol., 182, 290-296, (2000)
‣Modulators of tumor necrosis factor a production bearing dicarba-closo-dodecaborane as a hydrophobic pharmacophore
M. Tsuji, Y. Koiso, H. Takahashi, Y. Hashimoto, and Y. Endo
Biol. Pharm. Bull., 24, 513-516, (2000)
‣Structures of ADP-ribosylated rifampicin and its metabolite; Intermediates of rifampicin-ribosylation by Mycobacterium smegmatis DSM43756
N. Morisaki, Y. Hashimoto, K. Furihata, T. Imai, K. Watanabe, Y. Mikami, K. Yazawa, A. Ando, Y. Nagata, and E. R. Dabbs
J. Antibiotics, 53, 269-275, (2000)
‣Concise asymmetric synthesis of dysidiolode
M. Takahashi, K. Dodo, Y. Hashimoto, and R. Shirai
Tetrahedron Lett., 41, 2111-2114, (2000)
‣Synthesis of a novel class of cdc25A inhibitors from vitamin D3
K. Dodo, M. Takahashi, Y. Hashimoto, Y. Sugimoto, Y. Hashimoto and R. Shirai
Bioorg. Med. Chem. Lett., 10, 615-617, (2000)
‣Phosphorylation of unnatural phosphatidylinositols with phosphatidylinositol 3-kinase
N. Morisaki, K. Morita, A. Nishikawa, N. Nakatsu, Y. Fukui, Y. Hashimoto and R. Shirai
Tetrahedron, 56, 2603-2614, (2000)
‣Glyoxalase I is involvedin resistance of human leukemia cells to antitumor agent-induced apoptpsis
H. Sakamoto, T. Mashima, A. Kizaki, S. Dan, Y. Hashimoto, and T. Tsuruo
Blood, 95, 3214-321, (2000)
‣Novel α-glucosidase inhibitors with a tetrachlorophthalimide skeleton
S. Sou, S. Mayumi, H. Takahashi, R. Yamasaki, S. Kadoya, M. Sodeoka and Y. Hashimoto
Bioorg. Med. Chem. Lett., 10, 1081-1084, (2000)
‣Separation of phosphatidylinositol 4-phosphate from a mixture with phosphatidylserine and phosphtidylinositol by Sep-pak C18 cartrige
N. Morisaki, M. Masaoka, R. Shirai, and Y. Hashimoto
Biol. Pharm. Bull., 23, 1088-1089, (2000)
‣Identification of protein disulfide isomerase as a phorbol ester-binding protein
S. Mayumi, A. Azuma, H. Kobayashi, M. Sodeoka, K. Yano, S. Sugimoto, Y. Endo, and Y. Hashimoto
Biol. Pharm. Bull., 23, 1111-1113, (2000)
‣創薬のパラダイムシフト
橋本祐一
看護, 52, 92-95, (2000)
‣α-Glucosidase inhibitors with a phthalimide skeleton: Structure-activity relationship study
H. Takahashi, S. Sou, R. Yamasaki, M. Sodeoka, and Y. Hashimoto
Chem. Pharm. Bull. 48, 1494-1499, (2000)
‣Retinoidal pyrimidinecarboxylic acids. Unexpected diaza-substituent effects in retinobenzoic acids
K. Ohta, E. Kawachi, N. Inoue, H. Fukusawa, Y. Hashimoto, A. Itai, and H. Kagechika
Chem. Pharm. Bull., 48, 1504, (2000)
‣環状イミド構造を有する特異的アミノペプチダーゼ阻害剤リードの創製
高橋裕保,薦田正人,加来田博貴,橋本祐一
YAKUGAKU ZASSHI, 120, 909, (2000)
‣Bioprobes recognizing nucleic acids and signal transduction factors
Y. Hashimoto
Recent Rev. Devel. Organic Chem., 4, 87-120, (2000)
‣Anti-androgenic activity of substituted azo- and azoxy-benzene derivatives
H. Takahashi, T.Ishioka, Y. Koiso, M. Sodeoka, and Y. Hashimoto
Biol. Pharm. Bull., 23, 1387-1390, (2000)
1999
‣ADP-Ribosylation as an intermediate step in inactivation of rifampicin by a myco-bacterial gene
S. Quan, T. Imai, Y. Mikami, K. Yazawa, E. R. Dabbs, N. Morisaki, S. Iwasaki, Y. Hashimoto and K. Furihata
Antimicro. Agents Chemother., 43, 181-184, (1999)
‣Antiangiogenic activity of tumor necrosis factor-αproduction regulators derived from thalidomide
R. Shimazawa, H. Miyachi, H. Takayama, K. Kuroda, F. Kato, M. Kato and Y. Hashimoto
Biol. Pharm. Bull., 22, 224-226, (1999)
‣Non-peptide small-molecular inhibitors of dipeptidyl peptidase IV: N-phenylphthalimide analogs
R. Shimazawa, H. Takayama, F. Kato, M. Kato and Y. Hashimoto
Bioorg. Med. Chem. Lett., 9, 559-562, (1999)
‣The structural requirement of phosphatidylinositols as substrate of phosphatidylinositol 3-kinase
R. Shirai, K. Morita, A. Nishikawa, N. Nakatsu, Y. Fukui, N. Morisaki and Y. Hashimoto
Tetrahedron Lett., 40, 1693-1696, (1999)
‣Modification by heme oxygenase inhibitor, tin protoporphyrin, of cellular differentiation of human myeloid leukemia K562 cell line
Y. Koiso, Y. Fujimoto, D. Matsumura, O. Nakajima and Y. Hashimoto
Biol. Pharm. Bull., 22, 439-440, (1999)
‣Identification of a novel class of retinoic acid receptor β-selective retinoid antagonists and their inhibitory effects on AP-1 activity and retinoic acid-induced apoptosis in human breast cancer cells
Y. Li, Y. Hashimoto, A. Agadir, H. Kagechika and X. Zhang
J. Biol. Chem., 274, 15360-15366, (1999)
‣Novel small molecule nonpeptide aminopeptidase N inhibitors with a cyclic imide skeleton
R. Shimazawa, H. Takayama, Y. Fujimoto, M. Komoda, K. Dodo, R. Yamasaki, R. Shirai, Y. Koiso, K. Miyata, F. Kato, M. Kato, H. Miyachi and Y. Hashimoto
J. Enzyme Inhibition, 14, 259-275, (1999)
‣Potent homophthalimide-type inhibitors of B16F10/L5 mouse melanoma cell invasion
H. Kagechika, M. Komoda, Y. Fujimoto, Y. Koiso, H. Takayama, S. Kadoya, K. Miyata, F. Kato, M. Kato and Y. Hashimoto
Biol. Pharm. Bull., 22, 1010-1012, (1999)
‣Retinoid X receptor-antagonistic diazepinylbenzoic acids
M. Ebisawa, H. Umemiya, K. Ohta, H. Fukasawa, E. Kawachi, G. Christoffel, H. Gronemeyer, M. Tsuji, Y. Hashimoto, K. Shudo and K. Kagechika
Chem. Pharm. Bull., 47, 1778-1786, (1999)
‣Identification and characterization of a new intermediate in the ribosylative inactivation pathway of rifampin by Mycobacterium smegmatis
T. Imai, K. Watanabe, Y. Mikami, K. Yazawa, A. Ando, Y. Nagata, N. Morisaki, Y. Hashimoto, K. Furihata, E. R. Dabbs
Microbial Drug Resistance, 5, 259-264, (1999)
‣A new pregnane glycoside from Dioscorea collettii var. hypoglauca
K. Hu, X. S. Yao, A. J. Dong, H. Kobayashi, S. Iwasaki and Y. K. Jing
J. Nat. Prod., 62, 299-301, (1999)
‣Antineoplastic agents III: Steroidal glycosides from Solanum nigrum
K. Hu, H. Kobayashi, A. J. Dong, Y. K. Jing, S. Iwasaki and X. S. Yao
Planta Med., 65, 35-38, (1999)
‣サリドマイドをリードとした新規生物応答調節剤の創製
嶋澤るみ子, 高山久恵, 橋本祐一
有機合成化学協会誌, 57, 92-104, (1999)
‣サリドマイドによるサイトカインの生産制御とT細胞の機能修飾
橋本祐一
臨床免疫, 31, 577-583, (1999)
‣サイトカイニン特異的結合蛋白の分子同定
藤本康之, 永田龍二, 小林久芳, 首藤紘一, 橋本祐一
薬学雑誌, 119, 612-623, (1999)
‣らん藻Lyngbya majuscuraから単離された有糸分裂阻害剤Curacin Aの合成
白井隆一
有機合成協会誌, 57, 532-540, (1999)
‣がん細胞の分化誘導と核内レチノイン酸レセプター
橋本祐一
臨床腫瘍学第二版 (日本臨床腫瘍研究会編), p202-218, 癌と化学療法社, 東京, (1999)
‣がん と くすり
橋本祐一
東京化学同人, 東京, 全172頁, (1999)
1998
‣Photoaffinity labeling of RARs and mapping of labeled sites by an endoproteinase combination technique
Y. Hashimoto, and T. Sasaki
Methods in Molecular Biology, 89, 293-305, (1998)
‣Novel potent nonpeptide aminopeptidase N inhibitors with a cyclic imide skeleton
H. Miyachi, M. Kato, J. Kato, and Y. Hashimoto
J. Med. Chem., 41, 263-265, (1998)
‣レチノイドによるがんの治療と予防をめぐる話題
影近弘之, 萩本啓文, 森脇久隆, 橋本祐一(座談会)
ファルマシア, 34, 213-218, (1998)
‣Sequence selective interaction between nucleotides and intercalators bound to water soluble dextran: An application to the affinity chromatography of dinucleotides
R. Shirai, T. Ito, S. Iwasaki, and Y. Hashimoto
Nucleos. & Nucleot., 17, 593-601, (1998)
‣Isolation and structure of an antimitotic cyclic peptide, ustiloxin F: Chemical interrelation with homologous peptide, ustiloxin B
Y. Koiso, N. Morisaki, Y. Yamashita, Y. Mitsui, R. Shirai, Y. Hashimoto and S. Iwasaki
J. Antibiotics, 51, 418-422, (1998)
‣Synthesis and anti-tubulin activity of ustiloxin D derivatives
N. Morisaki, Y. Mitsui, Y. Yamashita, Y. Koiso, R. Shirai, Y. Hashimoto and S. Iwasaki
J. Antibiotics, 51, 423-427, (1998)
‣Specific detection of phosphatidylinositol 3,4,5-trisphosphate binding proteins by the PIP3 analogue beads: An application for rapid purification of the PIP3 binding proteins
T. Shirai, K. Tanaka, Y. Terada, T. Sawada, R. Shirai, Y. Hashimoto, S. Nagata, A. Iwamatsu, K.Okawa, S. Li, S. Hattori, H. Mono, Y. Fukui
Biochim. Biophys. Acta, 1402, 292-302, (1998)
‣Novel biological respose modifiers derived from thalidomide
Y. Hashimoto
Current Med. Chem., 5, 163-178, (1998)
‣Enhanced potency of perfluorinated thalodomide derivatives for inhibition of LPS-induced tumor necrosis factor-a production is associated with a change of mechanism of action
S. Niwayama, C. Loh, B. E. Turk, J. O. Liu, H. Miyachi and Y. Hashimoto
Bioorg. Med. Chem. Lett., 8, 1071-1076, (1998)
‣Potent retinoid synergists with a diphenylamine skeleton
K. Ohta, M. Tsuji, E. Kawachi, H. Fukasawa, Y. Hashimoto, K. Shudo and H. Kagechika
Biol. Pharm. Bull., 21, 544-546, (1998)
‣Novel thiazolidinedione derivatives with retinoid synergistic activity
M. Ebisawa, E. Kawachi, H. Fukasawa, Y. Hashimoto, A. Itai, K. Shudo and H. Kagechika
Biol. Pharm. Bull., 21, 547-549, (1998)
‣Tumor necrosis factor-alpha production enhancing activity of substituted 3'-methylthalidomide: Influence of substituents at the phthaloyl moiety on the activity and stereoselectivity
H. Miyachi, Y. Koiso, R. Shirai, S. Niwayama, J. O. Liu and Y. Hashimoto
Chem. Pharm. Bull., 46, 1165-1168, (1998)
‣Novel DNA minor groove binding with an aromatic layered structure
A. Tanatani, R. Fukutomi, H. Kakuta, N. Tomioka, A. Itai, Y. Hashimoto, K. Shudo and H. Kagechika
Nucleic Acids Symp. Ser., 39, 31-32, (1998)
‣Asymmetric synthesis of antimitotic combretadioxolane with potent antitumor activity against multi-drug registant cells
R. Shirai, H. Takayama, A. Nishikawa, Y. Koiso and Y. Hashimoto
Bioorg. Med. Chem. Letters 8, 1997-2000, (1998)
‣Aromatic layered guanidines bind sequence-specifically to DNA minor groove with precise fit
R. Fukutomi, A. Tanatani, H. Kakuta, N. Tomioka, A. Itai, Y. Hashimoto, K. Shudo and H. Kagechika
Tetrahedron Lett., 39, 6475-6778, (1998)
‣Synthesis of 6-amylsalicylic acid from 3-anisaldehyde: conversion of phthalide to thiophthalide by aluminium halide-butanethiol"
A. Nishikawa, Y. Hashimoto and R. Shirai
Tetrahedron Lett., 39, 7307-7308, (1998)
‣Synthesis of diacylglycerol analog of phosphatidylinositol 3,4,5-triphosphate
R. Shirai, K. Morita, A. Nishikawa, N. Nakatsu, Y. Fukui, N. Morisaki and Y. Hashimoto
Tetrahedron Lett., 39, 9485-9488, (1998)
‣Collisionally activated dissociation of 13-membered peptides, ustiloxins and phomopsins
N. Morisaki, Y. Koiso, Y. Mitsui, Y. Yamashita, H. Kobayashi, R. Shirai, Y. Hashimoto and S.Iwasaki
J. Mass Spectrom. Soc. Jpn., 46, 495-501, (1998)
‣Purification and cDNA cloning of cytokinin-specific binding protein from mung bean(Vigna radiata)
Y. Fujimoto, R. Nagata, H. Fukasawa, K. Yano, M. Azuma, A. Iida, S. Sugimoto, K. Shudo and Y.Hashimoto
Eur. J. Biochem., 258, 794-802, (1998)
‣生物活性発現の分子機構
橋本祐一
大学院講義有機化学,II巻,有機合成化学・生物有機化学, 野依良治・柴崎正勝・鈴木啓介・玉尾皓平・中筋一弘・奈良坂紘一編, 東京化学同人, p409-431, (1998)