Discovery of 6-N,N-bis(2,2,2-trifluoroethyl)amino- 4-trifluoromethylquinolin-2(1H)-one as a novel selective androgen receptor modulator.

Article Details

Citation

Copy to clipboard

van Oeveren A, Motamedi M, Mani NS, Marschke KB, Lopez FJ, Schrader WT, Negro-Vilar A, Zhi L

Discovery of 6-N,N-bis(2,2,2-trifluoroethyl)amino- 4-trifluoromethylquinolin-2(1H)-one as a novel selective androgen receptor modulator.

J Med Chem. 2006 Oct 19;49(21):6143-6.

PubMed ID

17034117 [ View in PubMed

]

Abstract

The androgen receptor is a member of the extended family of nuclear receptors and is widely distributed throughout the body. Androgen therapy is used to compensate for low levels of the natural hormones testosterone (T) and dihydrotestosterone and consists of administration of T, prodrugs thereof, or synthetic androgens. However, currently available androgens have many drawbacks. We identified 6-dialkylamino-4-trifluoromethylquinolin-2(1H)-ones as orally available tissue-selective androgen receptor modulators.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Stanolone	Androgen receptor	Ki (nM)	0.2	7.4	37	Details
Stanolone	Androgen receptor	EC 50 (nM)	5.1	7.4	37	Details