Discovery and SAR study of novel dihydroquinoline-containing glucocorticoid receptor agonists.
We have recently reported the discovery of a novel class of glucocorticoid receptor (GR) antagonists, exemplified by 3, containing a 1,2-dihydroquinoline molecular scaffold. Further SAR studies of these antagonists uncovered chemical modifications conveying agonist functional activity to this series. These agonists exhibit good GR binding affinity and are selective against other nuclear hormone receptors.
Boehringer Ingelheim Pharmaceuticals, Inc., 900 Ridgebury Road, Ridgefield, CT 06877, USA.
Hidenori
H
Takahashi
Younes
Y
Bekkali
Alison J
AJ
Capolino
Thomas
T
Gilmore
Susan E
SE
Goldrick
Paul V
PV
Kaplita
Lisa
L
Liu
Richard M
RM
Nelson
Donna
D
Terenzio
Ji
J
Wang
Ljiljana
L
Zuvela-Jelaska
John
J
Proudfoot
Gerald
G
Nabozny
David
D
Thomson
D011804:Quinolines / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D011965:Receptors, Glucocorticoid / Q000819:agonists* / Q000378:metabolism; D013329:Structure-Activity Relationship
D011804:Quinolines; D011965:Receptors, Glucocorticoid