Substituted 6-(1-pyrrolidine)quinolin-2(1H)-ones as novel selective androgen receptor modulators.
Article Details
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Martinborough E, Shen Y, Oeveren Av, Long YO, Lau TL, Marschke KB, Chang WY, Lopez FJ, Vajda EG, Rix PJ, Viveros OH, Negro-Vilar A, Zhi L
Substituted 6-(1-pyrrolidine)quinolin-2(1H)-ones as novel selective androgen receptor modulators.
J Med Chem. 2007 Oct 18;50(21):5049-52. Epub 2007 Sep 21.
- PubMed ID
- 17887661 [ View in PubMed]
- Abstract
The androgen receptor is a ligand inducible transcription factor that is involved in a broad range of physiological functions. Here we describe the discovery of a new class of orally available selective androgen receptor modulators. The lead compound, 6-[(2R,5R)-2-methyl-5-((R)-2,2,2-trifluoro-1-hydroxyethyl)pyrrolidin-1-yl]-4-trif luoromethylquinolin-2(1H)-one (6a), showed excellent anabolic activity in muscle with reduced effect on the prostate in a rat model of hypogonadism. The compound also improved bone strength in a rat model of post-menopausal osteoporosis.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Bicalutamide Androgen receptor Ki (nM) 70 7.4 37 Details Bicalutamide Androgen receptor IC 50 (nM) 128 7.4 37 Details LGD-2226 Androgen receptor Ki (nM) 4.6 7.4 37 Details LGD-2226 Androgen receptor EC 50 (nM) 0.2 7.4 37 Details LGD2941 Androgen receptor Ki (nM) 1.5 7.4 37 Details LGD2941 Androgen receptor EC 50 (nM) 7.1 7.4 37 Details Stanolone Androgen receptor Ki (nM) 0.2 7.4 37 Details Stanolone Androgen receptor EC 50 (nM) 5.1 7.4 37 Details