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
  • 1. Bristol-Myers Squibb Company, Research and Development, Princeton, NJ 08543-4000, USA. [email protected]
PMID: 20584610 DOI: 10.1016/j.bmcl.2010.06.034
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.