SYNTHESIS OF A STEROIDAL A-RING AROMATIC SULFONIC-ACID AS AN INHIBITOR OF STEROID 5-ALPHA-REDUCTASE

被引：17

作者：

HOLT, DA

OH, HJ

LEVY, MA

METCALF, BW

机构：

[1] Department of Medicinal Chemistry, SmithKline Beecham Pharmaceuticals, King of Prussia, PA

来源：

STEROIDS | 1991年 / 56卷 / 01期

关键词：

STEROIDS; STEROID; 5-ALPHA-REDUCTASE; ENZYME INHIBITION; BENIGN PROSTATIC HYPERPLASIA; SULFONIC ACID;

D O I：

10.1016/0039-128X(91)90106-6

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

The synthesis of 17-beta-(N,N-diisopropylcarbamoyl)estra-1,3,5(10)-triene-3-sulfonic acid (3) has been accomplished. Sulfonate 3 was designed as a novel inhibitor of human steroid 5-alpha-reductase based on considerations of enzyme mechanisms, and exhibits an inhibition constant in the low nanomolar range.

引用

页码：4 / 7

页数：4