A comparison of steroidal and non-steroidal inhibitors of human steroid 5 alpha-reductase: New tricyclic aryl acid inhibitors of the type-1 isozyme

被引：14

作者：

Abell, AD ^{[1
]}

Brandt, M ^{[1
]}

Levy, MA ^{[1
]}

Holt, DA ^{[1
]}

机构：

[1] SMITHKLINE BEECHAM PHARMACEUT,DEPT MED CHEM,KING OF PRUSSIA,PA 19406

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1996年 / 6卷 / 04期

关键词：

D O I：

10.1016/0960-894X(96)00054-6

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 9,10-dihydrophenanthrene-2-carboxylic acids has been prepared and evaluated in vitro as inhibitors of human recombinant steroid 5 alpha-reductase. 7-Bromo-9,10-dihydrophenanthrene-2-carboxylic acid, 8c, is a potent and selective non-steroidal inhibitor of human type-1 steroid 5 alpha-reductase (K-i,K-app 26 nM). The inhibitory activity relationships of steroidal and non-steroidal inhibitors, with 4-aza, 6-aza, diene acid, aryl acid and nitro-alkenes functionalities, are considered.

引用

页码：481 / 484

页数：4

共 23 条

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