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新型含磷17β-侧链米非司酮类似物作为孕激素受体拮抗剂。

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

作者信息

Jiang Weiqin, Allan George, Chen Xin, Fiordeliso James J, Linton Olivia, Tannenbaum Pamela, Xu Jun, Zhu Peifang, Gunnet Joseph, Demarest Keith, Lundeen Scott, Sui Zhihua

机构信息

Johnson & Johnson Pharmaceutical Research & Development L.L.C., Drug Discovery, Raritan, NJ 08869, USA.

出版信息

Steroids. 2006 Nov;71(11-12):949-54. doi: 10.1016/j.steroids.2006.07.003. Epub 2006 Aug 28.

Abstract

A novel series of steroidal compounds were designed and synthesized with various phosphorus-containing groups on the 17beta-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.

摘要

设计并合成了一系列新型甾体化合物,其17β-侧链带有各种含磷基团,作为孕酮受体拮抗剂。讨论了这些化合物的构效关系。对选定的化合物进行了大鼠孕酮敏感性试验。其中一些化合物比米非司酮更有效,在区分孕酮受体和糖皮质激素受体方面具有更好的选择性。

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