1589544-15-9Relevant academic research and scientific papers
Structure-Based Approach to Identify 5-[4-Hydroxyphenyl]pyrrole-2-carbonitrile Derivatives as Potent and Tissue Selective Androgen Receptor Modulators
Unwalla, Ray,Mousseau, James J.,Fadeyi, Olugbeminiyi O.,Choi, Chulho,Parris, Kevin,Hu, Baihua,Kenney, Thomas,Chippari, Susan,McNally, Christopher,Vishwanathan, Karthick,Kilbourne, Edward,Thompson, Catherine,Nagpal, Sunil,Wrobel, Jay,Yudt, Matthew,Morris, Carl A.,Powell, Dennis,Gilbert, Adam M.,Chekler, Eugene L. Piatnitski
supporting information, p. 6451 - 6457 (2017/08/02)
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.
Pyrroles versus cyclic nitrones: Catalyst-controlled divergent cyclization of N-(2-perfluoroalkyl-3-alkynyl) hydroxylamines
Zeng, Qin,Zhang, Li,Yang, Jieru,Xu, Bing,Xiao, Yuanjing,Zhang, Junliang
supporting information, p. 4203 - 4206 (2014/04/17)
The IPrAuNTf2/HNTf2 co-catalyzed cyclization of N-(2-perfluoroalkyl-3-alkynyl) hydroxylamines produces pyrroles in moderate to excellent yield, whereas the AgOTf-catalyzed reaction affords cyclic nitrones in high yields. the Partner
