3,3-diphenylpentane skeleton as a steroid skeleton substitute:: Novel inhibitors of human 5α-reductase 1

被引：13
作者：
Hosoda, Shinnosuke [1 ]
Hashimoto, Yuichi [1 ]
机构：
[1] Univ Tokyo, Inst Mol & Cellular Biosci, Bunkyo Ku, Tokyo 1130032, Japan
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 19期
基金：
日本学术振兴会;
关键词：
3,3-diphenylpentane; steroid; 5; alpha-reductase; inhibitor;
D O I：
10.1016/j.bmcl.2007.07.039
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
We designed and synthesized novel type 1 5 alpha-reductase inhibitors by using 3,3-diphenylpentane skeleton as a substitute for the usual steroid skeleton. 4-(3-(4-(N-Methylacetamido)phenyl)pentan-3-yl)phenyl dibenzylcarbamate (11k) is a competitive 5 alpha-reductase inhibitor with the IC50 value of 0.84 mu M. (C) 2007 Elsevier Ltd. All rights reserved.
引用
收藏
页码：5414 / 5418
页数：5
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