title: Development of progesterone receptor antagonists from 1,2-dihydrochromeno[3,4-f]quinoline agonist pharmacophore.
abstract: A series of 1,2-dihydrochromeno[3,4-f]quinoline derivatives was synthesized and tested in biological assays to evaluate the nonsteroidal progesterone receptor modulator pharmacophore (4) as antiprogestins. A number of potent analogues were identified by modification of the substituents at the D-ring.
authors.affiliation: Discovery Research, Ligand Pharmaceuticals, 10275 Science Center Drive, San Diego, CA 92121, USA. lzhi@ligand.com
authors.forename: Lin
authors.initials: L
authors.lastname: Zhi
authors.forename: Josef D
authors.initials: JD
authors.lastname: Ringgenberg
authors.forename: James P
authors.initials: JP
authors.lastname: Edwards
authors.forename: Christopher M
authors.initials: CM
authors.lastname: Tegley
authors.forename: Sarah J
authors.initials: SJ
authors.lastname: West
authors.forename: Barbara
authors.initials: B
authors.lastname: Pio
authors.forename: Mehrnouch
authors.initials: M
authors.lastname: Motamedi
authors.forename: Todd K
authors.initials: TK
authors.lastname: Jones
authors.forename: Keith B
authors.initials: KB
authors.lastname: Marschke
authors.forename: Dale E
authors.initials: DE
authors.lastname: Mais
authors.forename: William T
authors.initials: WT
authors.lastname: Schrader
mesh_terms: D000818:Animals; D002460:Cell Line; D002522:Chlorocebus aethiops; D006801:Humans; D020128:Inhibitory Concentration 50; D011374:Progesterone / Q000494:pharmacology; D011804:Quinolines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D011980:Receptors, Progesterone / Q000819:agonists / Q000037:antagonists & inhibitors* / Q000378:metabolism; D011987:Receptors, Steroid / Q000037:antagonists & inhibitors; D013329:Structure-Activity Relationship; D014158:Transcription, Genetic / Q000187:drug effects; D014162:Transfection
chemical_list: D011804:Quinolines; D011980:Receptors, Progesterone; D011987:Receptors, Steroid; D011374:Progesterone