title: Discovery of quinolines as selective glucocorticoid receptor agonists.
abstract: The dissociated glucocorticoid receptor (GR) agonist ZK 216348 is rendered GR-selective over other nuclear hormone receptors through replacing the methylbenzoxazine with a quinoline moiety. Compounds were shown to be efficacious in cell assays with respect to inflammation endpoints, along with reduced activity in a transactivation assay, hinting at an improved therapeutic window over corticosteroids.
authors: Medicinal Chemistry Berlin, Lead Generation & Optimization, Bayer Schering Pharma AG, Berlin D-13342, Germany. stefan.jaroch@bayerhealthcare.com
authors: Stefan
authors: S
authors: Jaroch
authors: Markus
authors: M
authors: Berger
authors: Christoph
authors: C
authors: Huwe
authors: Konrad
authors: K
authors: Krolikiewicz
authors: Hartmut
authors: H
authors: Rehwinkel
authors: Heike
authors: H
authors: Schäcke
authors: Norbert
authors: N
authors: Schmees
authors: Werner
authors: W
authors: Skuballa
mesh_terms: D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D002460:Cell Line; D004353:Drug Evaluation, Preclinical; D017930:Genes, Reporter / Q000235:genetics; D006801:Humans; D011804:Quinolines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D011965:Receptors, Glucocorticoid / Q000819:agonists* / Q000378:metabolism; D015533:Transcriptional Activation
chemical_list: D000893:Anti-Inflammatory Agents; D011804:Quinolines; D011965:Receptors, Glucocorticoid