A novel class of inhibitors for human steroid 5α-reductase:: Synthesis and biological evaluation of indole derivatives.: II

被引：0

作者：

Igarashi, S ^{[1
]}

Inami, H ^{[1
]}

Hara, H ^{[1
]}

Fujii, M ^{[1
]}

Koutoku, H ^{[1
]}

Oritani, H ^{[1
]}

Mase, T ^{[1
]}

机构：

[1] Yamanouchi Pharmaceut Co Ltd, Inst Drug Discovery Res, Tsukuba, Ibaraki 3058585, Japan

来源：

CHEMICAL & PHARMACEUTICAL BULLETIN | 2000年 / 48卷 / 03期

关键词：

5 alpha-reductase inhibitor; benign prostatic hypertrophy; indole derivative; YM-32906;

D O I：

暂无

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

In a search for novel nonsteroidal inhibitors of human prostatic 5 alpha-reductase, ne 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 acid (2d, YM-32906) showed more potent inhibitory activity than finasteride with an IC50 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 5 alpha-reductase with IC50 values of 2.1 and 73 nM, respectively. The synthesis and structure-activity relationships of these indole derivatives are presented.

引用

页码：382 / 388

页数：7