A NONSTEROIDAL DIENE ACID INHIBITOR OF HUMAN TYPE-2 STEROID 5-ALPHA-REDUCTASE

被引:16
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
关键词
D O I
10.1016/0960-894X(94)85034-8
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A series of 4a-methyl-3,4,4a,9-tetrahydrophenanthrene-2- carboxylic acids and 2-phosphinic acids has been prepared and evaluated in vitro as inhibitors of human recombinant steroid 5 alpha-reductase. 7-Chloro-4a-methyl-3,4,4a,9-tetrahydrophenanthrene-2- acid, 5, is a marginally selective inhibitor of human type 2 steroid Sa-reductase (K-i,K-app = 260 nM). The phosphinic acid compounds, 8 and 9, are weak inhibitors of types 1 and 2 steroid 5 alpha-reductase.
引用
收藏
页码:2327 / 2330
页数:4
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