1. Academic Validation
  2. Design and synthesis of 4-[3,5-dioxo-11-oxa-4,9-diazatricyclo[5.3.1.0(2,6)]undec-4-yl]-2-trifluoromethyl-benzonitriles as androgen receptor antagonists

Design and synthesis of 4-[3,5-dioxo-11-oxa-4,9-diazatricyclo[5.3.1.0(2,6)]undec-4-yl]-2-trifluoromethyl-benzonitriles as androgen receptor antagonists

  • Bioorg Med Chem Lett. 2010 Aug 1;20(15):4491-5. doi: 10.1016/j.bmcl.2010.06.034.
Hai-Yun Xiao 1 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 Jr Weifang Shan Ashvinikumar Gavai Mark E Salvati Gregory Vite
Affiliations

Affiliation

  • 1 Bristol-Myers Squibb Company, Research and Development, Princeton, NJ 08543-4000, USA. haiyun.xiao@bms.com
Abstract

A novel series of 4-[3,5-dioxo-11-oxa-4,9-diazatricyclo[5.3.1.0(2,6)]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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