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
Johnson & Johnson Pharmaceutical Research & Development L.L.C., Drug Discovery, Raritan, NJ 08869, USA.
Steroids. 2006 Nov;71(11-12):949-54. doi: 10.1016/j.steroids.2006.07.003. Epub 2006 Aug 28.
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.
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。
