The synthesis and evaluation of [2.2.1]-bicycloazahydantoins as androgen receptor antagonists

  • Bioorg Med Chem Lett. 2004 Dec 20;14(24):6107-11. doi: 10.1016/j.bmcl.2004.09.049.
Aaron Balog  1 ,  Mark E Salvati ,  Weifang Shan ,  Arvind Mathur ,  Leslie W Leith ,  Donna D Wei ,  Ricardo M Attar ,  Jieping Geng ,  Cheryl A Rizzo ,  Chihuei Wang ,  Stanley R Krystek ,  John S Tokarski ,  John T Hunt ,  Marco Gottardis ,  Roberto Weinmann
Affiliations
  • 1. Department of Oncology Chemistry, Bristol-Myers Squibb Pharmaceutical Research Institute, PO Box 4000, Princeton, NJ 08543-4000, USA. [email protected]
PMID: 15546739 DOI: 10.1016/j.bmcl.2004.09.049
Abstract

A novel series of [2.2.1]-azahydantoins has been designed and synthesized in an enantiospecific manner. The ability of these compounds to act as antagonists to the Androgen Receptor was investigated and several were found to have potent activity in vitro.