Synthesis and biological evaluation of 4-(4-(Alkyl- and phenylaminocarbonyl)benzoyl)benzoic acid derivatives as non-steroidal inhibitors of steroid 5α-reductase isozymes 1 and 2

被引：0
|
作者：
Salem, OIA [1 ]
Schulz, T [1 ]
Hartmann, RW [1 ]
机构：
[1] Univ Saarland, D-66041 Saarbrucken, Germany
来源：
ARCHIV DER PHARMAZIE | 2002年 / 335卷 / 2-3期
关键词：
non-steroidal 5 alpha-reductase inhibitors; substituted benzoylbenzoic acids; rat and human steroid 5 alpha-reductase isozymes 1 and 2; benign prostatic hyperplasia; prostate cancer;
D O I：
10.1002/1521-4184(200203)335:2/3<83::AID-ARDP83>3.0.CO;2-3
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
The synthesis and biological evaluation of 4-(4-(alkyl- and phenylaminocarbonyl)benzoyl)benzoic acids (4a-4d) as non-steroidal inhibitors of steroid 5alpha-reductase are described. The compounds were tested in vitro for inhibitory activity toward rat and human 5alpha-reductase isozymes 1 and 2 at a concentration of 10 muM. The most active inhibitor for the human type 2 isozyme was 4-(4-(phenylaminocarbonyl)benzoyl)benzoic acid, compound 4c (IC50 = 0.82 muM).
引用
收藏
页码：83 / 88
页数：6
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