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.
Takahashi
Hidenori
H
Boehringer Ingelheim Pharmaceuticals, Inc., 900 Ridgebury Road, Ridgefield, CT 06877, USA.
Bekkali
Younes
Y
Capolino
Alison J
AJ
Gilmore
Thomas
T
Goldrick
Susan E
SE
Kaplita
Paul V
PV
Liu
Lisa
L
Nelson
Richard M
RM
Terenzio
Donna
D
Wang
Ji
J
Zuvela-Jelaska
Ljiljana
L
Proudfoot
John
J
Nabozny
Gerald
G
Thomson
David
D
D011804:Quinolines / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D011965:Receptors, Glucocorticoid / Q000819:agonists* / Q000378:metabolism; D013329:Structure-Activity Relationship
D011804:Quinolines; D011965:Receptors, Glucocorticoid