Journal of Medicinal Chemistry p. 4918 - 4926 (2015)
Update date:2022-08-15
Topics:
Eda, Masahiro
Kuroda, Tomoko
Kaneko, Satoshi
Aoki, Yoshiyuki
Yamashita, Masami
Okumura, Chieko
Ikeda, Yoshitaka
Ohbora, Tomoko
Sakaue, Masaki
Koyama, Natsumi
Aritomo, Keiichi
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.
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