A Novel Class of Inhibitors for Human Steroid 5α-Reductase : Synthesis and Biological Evaluation of Indole Derivatives. II

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概要

• 論文の詳細を見る

• In a search for novel nonsteroidal inhibitors of human prostatic 5α-reductase, we found a new series of indole derivatives that showed potent inhibitory activities for the human enzyme. Among them, 4-[(1-benzyl-1H-indol-5-yl)oxy]-3-chlorobenzoic aicd (2d, YM-32906) showed more potent inhibitory activity than finasteride with an IC_<50> value of 0.44 nM. 3-Chloro-4-{[1-(4-phenoxybenzyl)-1H-indol-5-yl]oxy}benzoic acid (2m) showed inhibitory activities for both human and rat prostatic 5α-reductase with IC_<50> values of 2.1 and 73 nM, respectively. The synthesis and structure-activity relationships of these indole derivatives are presented.

• 公益社団法人日本薬学会の論文
• 2000-03-01

著者

• Hara Hideaki

  Research And Development Center Santen Pharmaceutical Co. Ltd.

• Fujii M

  Samsung Yokohama Res. Inst. Co. Ltd. Yokohama‐shi Jpn

• Fujii M

  Tokyo University Of Science:(present Office)utsunomiya University

• Fujii M

  Yamanouchi Pharmaceutical Co. Ltd. Ibaraki Jpn

• Fujii M

  Showa Univ. Tokyo Jpn

• IGARASHI Susumu

  Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd.,

• INAMI Hiroshi

  Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd.,

• HARA Hiromu

  (Present Address)Secretariat Dept., Yamanouchi Pharmaceutical Co., Ltd.,

• FUJII Masahiro

  Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd.,

• KOUTOKU Hiroshi

  Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd.,

• ORITANI Hiroyuki

  (Present address)Institute for Drug Development Research, Yamanouchi Pharmaceutical Co., Ltd.,

• MASE Toshiyasu

  (Present address)Bulk Manufacturing & Technology Division, Yamanouchi Pharmaceutical Co., Ltd.,

• Igarashi S

  Department Of Materials Science. Facnlty Of Engineering Ibaraki University

• Inami Hiroshi

  Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.

• Hara H

  (present Address)corporate Planning Dept. Yamanouchi Pharmaceutical Co. Ltd.

• Mase T

  Yamanouchi Pharmaceutical Co. Ltd. Ibaraki Jpn

• Koutoku Hiroshi

  Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.

• Oritani Hiroyuki

  (present Address)institute For Drug Development Research Yamanouchi Pharmaceutical Co. Ltd.

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