کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1362992 | 981500 | 2010 | 4 صفحه PDF | دانلود رایگان |
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.
The dissociated glucocorticoid receptor (GR) agonist ZK 216348 (1) is rendered GR-selective by replacing the methylbenzoxazine moiety with quinolines. Compounds were shown to be efficacious in vitro in reporter gene and cell assays, along with reduced activity in a transactivation assay, hinting at an improved therapeutic window over corticosteroids.Figure optionsDownload as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 20, Issue 19, 1 October 2010, Pages 5835–5838