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

Article Details

Citation

Balog A, Salvati ME, Shan W, Mathur A, Leith LW, Wei DD, Attar RM, Geng J, Rizzo CA, Wang C, Krystek SR, Tokarski JS, Hunt JT, Gottardis M, Weinmann R

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

Bioorg Med Chem Lett. 2004 Dec 20;14(24):6107-11.

PubMed ID
15546739 [ View in PubMed
]
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.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
BicalutamideAndrogen receptorIC 50 (nM)170N/AN/ADetails
BicalutamideAndrogen receptorKi (nM)65N/AN/ADetails
BicalutamideAndrogen receptorIC 50 (nM)400N/AN/ADetails