Novel phosphorus-containing 17β-side chain mifepristone analogues as progesterone receptor antagonists

被引：24

作者：

Jiang, Weiqin ^{[1
]}

Allan, George ^{[1
]}

Chen, Xin ^{[1
]}

Fiordeliso, James J. ^{[1
]}

Linton, Olivia ^{[1
]}

Tannenbaum, Pamela ^{[1
]}

Xu, Jun ^{[1
]}

Zhu, Peifang ^{[1
]}

Gunnet, Joseph ^{[1
]}

Demarest, Keith ^{[1
]}

Lundeen, Scott ^{[1
]}

Sui, Zhihua ^{[1
]}

机构：

[1] Johnson & Johnson Pharmaceut Res & Dev LLC, Drug Discovery, Raritan, NJ 08869 USA

来源：

STEROIDS | 2006年 / 71卷 / 11-12期

关键词：

C-17 phosphorus-containing steroids; selective progesterone receptor antagonist;

D O I：

10.1016/j.steroids.2006.07.003

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：

A novel series of steroidal compounds were designed and synthesized with various phosphorus-containing groups on the 17 beta-side chain as progesterone receptor antagonists. The structure -activity relationships of these compounds are discussed. Selected compounds were tested in an rat progesterone-sensitive assay. Some of these compounds are more potent than mifepristone, with a better selectivity profile in differentiating progesterone receptor from glucocorticoid receptor. (C) 2006 Elsevier Inc. All rights reserved.

引用

页码：949 / 954

页数：6

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