Download MendeleyStructure-Based Approach To Identify 5-[4-Hydroxyphenyl]pyrrole-2-carbonitrile Derivatives as Potent and Tissue Selective Androgen Receptor Modulators.
Unwalla, R., Mousseau, J.J., Fadeyi, O.O., Choi, C., Parris, K., Hu, B., Kenney, T., Chippari, S., McNally, C., Vishwanathan, K., Kilbourne, E., Thompson, C., Nagpal, S., Wrobel, J., Yudt, M., Morris, C.A., Powell, D., Gilbert, A.M., Chekler, E.L.P.(2017) J Med Chem 60: 6451-6457
- PubMed: 28696695
- DOI: https://doi.org/10.1021/acs.jmedchem.7b00373
- Primary Citation of Related Structures:
5VO4 - PubMed Abstract:
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 EC 50 = 0.34 nM) and selective (N/C interaction EC 50 = 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.
Organizational Affiliation:
Pfizer Worldwide Research & Development , 610 Main Street, Cambridge, Massachusetts 02139, United States.
