title: Discovery and SAR study of novel dihydroquinoline containing glucocorticoid receptor ligands.
abstract: 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.
authors.affiliation: Boehringer Ingelheim Pharmaceuticals, Inc., 900 Ridgebury Road, Ridgefield, CT 06877, USA. htakahas@rdg.boehringer-ingelheim.com
authors.forename: Hidenori
authors.initials: H
authors.lastname: Takahashi
authors.forename: Younes
authors.initials: Y
authors.lastname: Bekkali
authors.forename: Alison J
authors.initials: AJ
authors.lastname: Capolino
authors.forename: Thomas
authors.initials: T
authors.lastname: Gilmore
authors.forename: Susan E
authors.initials: SE
authors.lastname: Goldrick
authors.forename: Richard M
authors.initials: RM
authors.lastname: Nelson
authors.forename: Donna
authors.initials: D
authors.lastname: Terenzio
authors.forename: Ji
authors.initials: J
authors.lastname: Wang
authors.forename: Ljiljana
authors.initials: L
authors.lastname: Zuvela-Jelaska
authors.forename: John
authors.initials: J
authors.lastname: Proudfoot
authors.forename: Gerald
authors.initials: G
authors.lastname: Nabozny
authors.forename: David
authors.initials: D
authors.lastname: Thomson
mesh_terms: 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
chemical_list: 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