Simple bi- and tricyclic inhibitors of human steroid 5α-reductase

被引：11

作者：

Abell, AD ^{[1
]}

Prince, MJ

McNulty, AM

Neubauer, BL

机构：

[1] Univ Canterbury, Dept Chem, Christchurch 1, New Zealand

[2] Lilly Res Labs, Indianapolis, IN 46285 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 17期

关键词：

D O I：

10.1016/S0960-894X(00)00368-1

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A number of tricyclic thiolactams, bicyclic lactams, and bicyclic thiolactams have been prepared and evaluated in vitro as inhibitors of types and ? steroid 5 alpha-reductase. The tricycles with an 8-chloro substituent in the C-ring are nM (IC50) inhibitors of type steroid 5 alpha-reductase (SR). In all the cases studied, lactams are more potent than the corresponding thiolactams. Activity against type 2 SR is greatly enhanced by a styryl (or ate) substituent on the aryl ring of the tri- and bicycles and also a related tricyclic aryl acid. (C) 2000 Elsevier Science Ltd. All rights reserved.

引用

页码：1909 / 1911

页数：3

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