SYNTHESIS AND EVALUATION OF 3-CARBOXYMETHYL STEROIDS AS INHIBITORS OF HUMAN PROSTATIC STEROID 5-ALPHA-REDUCTASE

被引:6
|
作者
HOLT, DA
OH, HJ
ROZAMUS, LW
YEN, HK
BRANDT, M
LEVY, MA
METCALF, BW
机构
[1] Department of Medicinal Chemistry, SmithKline Beecham Pharmaceuticals, King of Prussia, PA 19406-0939
关键词
D O I
10.1016/S0960-894X(00)80052-9
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A series of 3-carboxymethyl steroids has been prepared and assayed in vitro as inhibitors of steroid 5alpha-reductase isolated from human prostatic tissue. Potent inhibition was observed with analogs from both androstene and estratriene families. Phosphonic and sulfonic acid analogs were also prepared and found to lack significant inhibitory activity.
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页码:1735 / 1738
页数:4
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