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

Aaron Balog; 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

doi:10.1016/j.bmcl.2004.09.049

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.

Authors

Aaron Balog¹, 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

Affiliation

¹ Department of Oncology Chemistry, Bristol-Myers Squibb Pharmaceutical Research Institute, PO Box 4000, Princeton, NJ 08543-4000, USA. aaron.balog@bms.com

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.

MeSH terms

Androgen Receptor Antagonists*
Aza Compounds / chemical synthesis*
Aza Compounds / chemistry
Aza Compounds / pharmacology*
Cell Line
Cell Survival / drug effects
Drug Design
Drug Evaluation, Preclinical
Evaluation Studies as Topic
Humans
Hydantoins / chemical synthesis*
Hydantoins / chemistry
Hydantoins / pharmacology*
Models, Molecular
Molecular Conformation
Structure-Activity Relationship

Substances

Androgen Receptor Antagonists
Aza Compounds
Hydantoins