4.7 Article Proceedings Paper

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

Journal

JOURNAL OF MEDICINAL CHEMISTRY
Volume 49, Issue 21, Pages 6143-6146

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/jm060792t

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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.

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