Development of progesterone receptor antagonists from 1,2-dihydrochromeno[3,4-f]quinoline agonist pharmacophore.
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.
Zhi
Lin
L
Discovery Research, Ligand Pharmaceuticals, 10275 Science Center Drive, San Diego, CA 92121, USA. lzhi@ligand.com
Ringgenberg
Josef D
JD
Edwards
James P
JP
Tegley
Christopher M
CM
West
Sarah J
SJ
Pio
Barbara
B
Motamedi
Mehrnouch
M
Jones
Todd K
TK
Marschke
Keith B
KB
Mais
Dale E
DE
Schrader
William T
WT
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
D011804:Quinolines; D011980:Receptors, Progesterone; D011987:Receptors, Steroid; D011374:Progesterone