title: Novel phosphorus-containing 17beta-side chain mifepristone analogues as progesterone receptor antagonists.
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.
authors.affiliation: Johnson & Johnson Pharmaceutical Research & Development L.L.C., Drug Discovery, Raritan, NJ 08869, USA. wjiang1@prdus.jnj.com
authors.forename: Weiqin
authors.initials: W
authors.lastname: Jiang
authors.forename: George
authors.initials: G
authors.lastname: Allan
authors.forename: Xin
authors.initials: X
authors.lastname: Chen
authors.forename: James J
authors.initials: JJ
authors.lastname: Fiordeliso
authors.forename: Olivia
authors.initials: O
authors.lastname: Linton
authors.forename: Pamela
authors.initials: P
authors.lastname: Tannenbaum
authors.forename: Jun
authors.initials: J
authors.lastname: Xu
authors.forename: Peifang
authors.initials: P
authors.lastname: Zhu
authors.forename: Joseph
authors.initials: J
authors.lastname: Gunnet
authors.forename: Keith
authors.initials: K
authors.lastname: Demarest
authors.forename: Scott
authors.initials: S
authors.lastname: Lundeen
authors.forename: Zhihua
authors.initials: Z
authors.lastname: Sui
mesh_terms: D000818:Animals; D001665:Binding Sites; D002460:Cell Line; D005260:Female; D006727:Hormone Antagonists / Q000737:chemistry* / Q000378:metabolism; D006801:Humans; D015735:Mifepristone / Q000737:chemistry* / Q000378:metabolism; D015394:Molecular Structure; D010758:Phosphorus / Q000737:chemistry*; D011374:Progesterone / Q000737:chemistry / Q000378:metabolism; D051381:Rats; D017207:Rats, Sprague-Dawley; D011980:Receptors, Progesterone / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
chemical_list: D006727:Hormone Antagonists; D011980:Receptors, Progesterone; D010758:Phosphorus; D015735:Mifepristone; D011374:Progesterone