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.

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