3 years ago

Structure-Based Approach To Identify 5-[4-Hydroxyphenyl]pyrrole-2-carbonitrile Derivatives as Potent and Tissue Selective Androgen Receptor Modulators

Structure-Based Approach To Identify 5-[4-Hydroxyphenyl]pyrrole-2-carbonitrile Derivatives as Potent and Tissue Selective Androgen Receptor Modulators
Carl A. Morris, Baihua Hu, Edward Kilbourne, Dennis Powell, Kevin Parris, James J. Mousseau, Sunil Nagpal, Adam M. Gilbert, Matthew Yudt, Karthick Vishwanathan, Susan Chippari, Chulho Choi, Olugbeminiyi O. Fadeyi, Jay Wrobel, Catherine Thompson, Christopher McNally, Thomas Kenney, Eugene L. Piatnitski Chekler, Ray Unwalla
In an effort to find new and safer treatments for osteoporosis and frailty, we describe a novel series of selective androgen receptor modulators (SARMs). Using a structure-based approach, we identified compound 7, a potent AR (ARE EC50 = 0.34 nM) and selective (N/C interaction EC50 = 1206 nM) modulator. In vivo data, an AR LBD X-ray structure of 7, and further insights from modeling studies of ligand receptor interactions are also presented.

Publisher URL: http://dx.doi.org/10.1021/acs.jmedchem.7b00373

DOI: 10.1021/acs.jmedchem.7b00373

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