Discovery and SAR study of novel dihydroquinoline containing glucocorticoid receptor ligands.
We report the discovery of a novel class of glucocorticoid receptor (GR) ligands based on 1,2-dihydroquinoline molecular scaffold. The compounds exhibit good GR binding affinity and selectivity profile against other nuclear hormone receptors.
Takahashi
Hidenori
H
Boehringer Ingelheim Pharmaceuticals, Inc., 900 Ridgebury Road, Ridgefield, CT 06877, USA. htakahas@rdg.boehringer-ingelheim.com
Bekkali
Younes
Y
Capolino
Alison J
AJ
Gilmore
Thomas
T
Goldrick
Susan E
SE
Nelson
Richard M
RM
Terenzio
Donna
D
Wang
Ji
J
Zuvela-Jelaska
Ljiljana
L
Proudfoot
John
J
Nabozny
Gerald
G
Thomson
David
D
D000893:Anti-Inflammatory Agents / Q000494:pharmacology; D003907:Dexamethasone / Q000494:pharmacology; D006367:HeLa Cells; D006801:Humans; D007375:Interleukin-1 / Q000494:pharmacology; D015850:Interleukin-6 / Q000378:metabolism; D008024:Ligands; D008324:Mammary Tumor Virus, Mouse / Q000235:genetics; D008958:Models, Molecular; D015394:Molecular Structure; D011401:Promoter Regions, Genetic / Q000187:drug effects; D011804:Quinolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D011960:Receptors, Estrogen / Q000187:drug effects / Q000378:metabolism; D011965:Receptors, Glucocorticoid / Q000037:antagonists & inhibitors* / Q000378:metabolism*; D018161:Receptors, Mineralocorticoid / Q000187:drug effects / Q000378:metabolism; D011980:Receptors, Progesterone / Q000187:drug effects / Q000378:metabolism; D013329:Structure-Activity Relationship; D014158:Transcription, Genetic / Q000187:drug effects; D015533:Transcriptional Activation / Q000187:drug effects / Q000235:genetics
D000893:Anti-Inflammatory Agents; D007375:Interleukin-1; D015850:Interleukin-6; D008024:Ligands; D011804:Quinolines; D011960:Receptors, Estrogen; D011965:Receptors, Glucocorticoid; D018161:Receptors, Mineralocorticoid; D011980:Receptors, Progesterone; D003907:Dexamethasone