title: Nonsteroidal progesterone receptor antagonists based on a conformationally-restricted subseries of 6-aryl-1,2-dihydro-2,2,4-trimethylquinolines.
abstract: A series of nonsteroidal human progesterone receptor (hPR) antagonists based on conformationally-restricted analogues of a 6-aryl-1,2-dihydro-2,2,4-trimethylquinoline pharmacophore were synthesized and evaluated for their ability to bind to the human progesterone receptor and inhibit progesterone-stimulated reporter gene expression in mammalian cells.
authors.affiliation: Department of Medicinal Chemistry, Ligand Pharmaceuticals, San Diego, CA 92121, USA.
authors.forename: L G
authors.initials: LG
authors.lastname: Hamann
authors.forename: D T
authors.initials: DT
authors.lastname: Winn
authors.forename: C L
authors.initials: CL
authors.lastname: Pooley
authors.forename: C M
authors.initials: CM
authors.lastname: Tegley
authors.forename: S J
authors.initials: SJ
authors.lastname: West
authors.forename: L J
authors.initials: LJ
authors.lastname: Farmer
authors.forename: L
authors.initials: L
authors.lastname: Zhi
authors.forename: J P
authors.initials: JP
authors.lastname: Edwards
authors.forename: K B
authors.initials: KB
authors.lastname: Marschke
authors.forename: D E
authors.initials: DE
authors.lastname: Mais
authors.forename: M E
authors.initials: ME
authors.lastname: Goldman
authors.forename: T K
authors.initials: TK
authors.lastname: Jones
mesh_terms: D006801:Humans; D008968:Molecular Conformation; D011804:Quinolines / Q000737:chemistry* / Q000494:pharmacology*; D011980:Receptors, Progesterone / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
chemical_list: D011804:Quinolines; D011980:Receptors, Progesterone