Design and synthesis of 4-[3,5-dioxo-11-oxa-4,9-diazatricyclo[5.3.1.02,6]undec-4-yl]-2-trifluoromethyl-benzonitriles as androgen receptor antagonists |
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| Authors: | Hai-Yun Xiao Aaron Balog Ricardo M Attar David Fairfax Linda B Fleming Christian L Holst Gregory S Martin Lana M Rossiter Jing Chen Mary-Ellen Cvjic Janet Dell-John Jieping Geng Marco M Gottardis Wen-Ching Han Andrew Nation Mary Obermeier Cheryl A Rizzo Liang Schweizer Thomas Spires Weifang Shan Gregory Vite |
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| Institution: | 1. Bristol-Myers Squibb Company, Research and Development, Princeton, NJ 08543-4000, USA;2. Albany Molecular Research Institute, Albany, NY 12203, USA |
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| Abstract: | A novel series of 4-3,5-dioxo-11-oxa-4,9-diazatricyclo5.3.1.02,6]undec-4-yl]-2-trifluoromethyl-benzonitriles has been synthesized. The ability of these compounds to act as antagonists of the androgen receptor was investigated and several were found to have potent activity in vitro and in vivo. |
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