Nonsteroidal progesterone receptor antagonists based on a conformationally-restricted subseries of 6-aryl-1,2-dihydro-2,2,4-trimethylquinolines.
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.
Hamann
L G
LG
Department of Medicinal Chemistry, Ligand Pharmaceuticals, San Diego, CA 92121, USA.
Winn
D T
DT
Pooley
C L
CL
Tegley
C M
CM
West
S J
SJ
Farmer
L J
LJ
Zhi
L
L
Edwards
J P
JP
Marschke
K B
KB
Mais
D E
DE
Goldman
M E
ME
Jones
T K
TK
D006801:Humans; D008968:Molecular Conformation; D011804:Quinolines / Q000737:chemistry* / Q000494:pharmacology*; D011980:Receptors, Progesterone / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
D011804:Quinolines; D011980:Receptors, Progesterone