A Novel Class of Inhibitors for Human and Rat Steroid 5α-Reductases : Synthesis and Biological Evaluation of Indoline and Aniline Derivatives. III
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概要
- 論文の詳細を見る
While searching for novel nonsteroidal inhibitors of human and rat prostatic 5α-reductases, we found a new series of indoline and aniline derivatives that showed potent inhibitory activities for both enzymes. Among them, 3-chloro-4-{1-(4-phenoxybenzyl)indolin-5-yl]oxy}benzoic acid (2e, YM-36117) showed a more portent inhibitory activity for the human enzyme than ONO-3805 with an IC_<50> value of 5.3 nM and a reduced rat prostatic dihydrotestosterone (DHT) concentration by oral administration. The synthesis and the structure-activity relationships of these indoline and aniline derivatives are presented.
- 公益社団法人日本薬学会の論文
- 2000-11-01
著者
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Hara Hideaki
Research And Development Center Santen Pharmaceutical Co. Ltd.
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IGARASHI Susumu
Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd.,
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INAMI Hiroshi
Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd.,
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HARA Hiromu
(Present Address)Secretariat Dept., Yamanouchi Pharmaceutical Co., Ltd.,
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KOUTOKU Hiroshi
Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd.,
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ORITANI Hiroyuki
(Present address)Institute for Drug Development Research, Yamanouchi Pharmaceutical Co., Ltd.,
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MASE Toshiyasu
(Present address)Bulk Manufacturing & Technology Division, Yamanouchi Pharmaceutical Co., Ltd.,
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Igarashi S
Department Of Materials Science. Facnlty Of Engineering Ibaraki University
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Inami Hiroshi
Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.
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Hara H
(present Address)corporate Planning Dept. Yamanouchi Pharmaceutical Co. Ltd.
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Mase T
Yamanouchi Pharmaceutical Co. Ltd. Ibaraki Jpn
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Koutoku Hiroshi
Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.
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Oritani Hiroyuki
(present Address)institute For Drug Development Research Yamanouchi Pharmaceutical Co. Ltd.
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