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

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. doi: 10.1021/jm060792t.
Arjan van Oeveren 1,  Mehrnouch Motamedi,  Neelakandha S Mani,  Keith B Marschke,  Francisco J López,  William T Schrader,  Andrés Negro-Vilar,  Lin Zhi
Affiliations

Affiliation

  • 1 Discovery Research, Ligand Pharmaceuticals Inc., 10275 Science Center Drive, San Diego, California 92121, USA. avanoeveren@ligand.com
PMID: 17034117 DOI: 10.1021/jm060792t
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.

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