INHIBITION OF STEROID 5-ALPHA-REDUCTASE BY 3-NITROSTEROIDS - SYNTHESIS, MECHANISM OF INHIBITION, AND INVIVO ACTIVITY

被引：24

作者：

HOLT, DA ^{[1
]}

LEVY, MA ^{[1
]}

YEN, HK ^{[1
]}

OH, HJ ^{[1
]}

METCALF, BW ^{[1
]}

WIER, PJ ^{[1
]}

机构：

[1] SMITHKLINE BEECHAM PHARMACEUT,DEPT INVEST TOXICOL,KING OF PRUSSIA,PA 19406

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1991年 / 1卷 / 01期

关键词：

D O I：

10.1016/S0960-894X(01)81084-2

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of A-ring unsaturated 3-nitrosteroids has been prepared and assayed in vitro as inhibitors of steroid 5-alpha-reductase. One of these compounds, 3-nitro-5-alpha-androst-3-ene-17-beta-diisopropylcarboxamide (4), inhibits the human enzyme with a K(i) of 50 nM and exhibits competitive inhibition versus testosterone. Potent oral activity of 4 was demonstrated in cynomolgus monkeys.

引用

页码：27 / 32

页数：6

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