Synthesis and Biological Evaluation of Cyclopentaquinoline Derivatives as Nonsteroidal Glucocorticoid Receptor Antagonists.
Basic Information
ID: ALA3580565
Journal: J Med Chem
Title: Synthesis and Biological Evaluation of Cyclopentaquinoline Derivatives as Nonsteroidal Glucocorticoid Receptor Antagonists.
Authors: Eda M, Kuroda T, Kaneko S, Aoki Y, Yamashita M, Okumura C, Ikeda Y, Ohbora T, Sakaue M, Koyama N, Aritomo K.
Abstract: The steroidal glucocorticoid antagonist mifepristone has been reported to improve the symptoms of depression. We report the discovery of 6-(3,5-dimethylisoxazol-4-yl)-2,2,4,4-tetramethyl-2,3,4,7,8,9-hexahydro-1H-cyclopenta[h]quinolin-3-one 3d (QCA-1093) as a novel nonsteroidal glucocorticoid receptor antagonist. The compound displayed potent in vitro activity, high selectivity over other steroid hormone receptors, and significant antidepressant-like activity in vivo.
CiteXplore: 25978072
DOI: 10.1021/jm501758q
Patent ID: ┄