New progesterone receptor antagonists:: Phosphorus-containing 11β-aryl-substituted steroids

被引：54

作者：

Jiang, Weiqin ^{[1
]}

Allan, George ^{[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：

BIOORGANIC & MEDICINAL CHEMISTRY | 2006年 / 14卷 / 19期

关键词：

phosphorus-containing steroids; progesterone receptor antagonist;

D O I：

10.1016/j.bmc.2006.05.066

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 new series of phosphorus-containing 11 beta-aryl-substituted steroids have been synthesized in an eight-step sequence involving a palladium-catalyzed coupling reaction to introduce a phosphorus group onto the aromatic ring. The compounds were evaluated for progesterone receptor (PR) antagonist activity in a T47D cell-based assay and for glucocorticoid receptor (GR) antagonist activity in an A549 cell-based assay. The structure-activity relationships of these compounds are discussed. Selected compounds were tested in vivo in a rat complement C3 assay. (c) 2006 Elsevier Ltd. All rights reserved.

引用

页码：6726 / 6732

页数：7

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