Discovery of BMS-641988, a Novel Androgen Receptor Antagonist for the Treatment of Prostate Cancer.

BMS-641988 (23) is a novel, nonsteroidal androgen receptor antagonist designed for the treatment of prostate cancer. The compound has high binding affinity for the AR and acts as a functional antagonist in vitro.

BMS-641988 is efficacious in multiple human prostate cancer xenograft models, including CWR22-BMSLD1 where it displays superior efficacy relative to bicalutamide. Based on its promising preclinical profile, BMS-641988 was selected for clinical development.

ACS medicinal chemistry letters 2015 Jun 19*** epublish ***

Aaron Balog, Richard Rampulla, Gregory S Martin, Stanley R Krystek, Ricardo Attar, Janet Dell-John, John D DiMarco, David Fairfax, Jack Gougoutas, Christian L Holst, Andrew Nation, Cheryl Rizzo, Lana M Rossiter, Liang Schweizer, Weifang Shan, Steven Spergel, Thomas Spires, Georgia Cornelius, Marco Gottardis, George Trainor, Gregory D Vite, Mark E Salvati

Bristol Myers-Squibb Research and Development , Princeton, New Jersey 08543, United States , Bristol Myers-Squibb Research and Development , Princeton, New Jersey 08543, United States , Albany Molecular Research Inc , 21 Corporate Circle, Albany, New York 12203, United States , Bristol Myers-Squibb Research and Development , Princeton, New Jersey 08543, United States , Bristol Myers-Squibb Research and Development , Princeton, New Jersey 08543, United States , Bristol Myers-Squibb Research and Development , Princeton, New Jersey 08543, United States , Bristol Myers-Squibb Research and Development , Princeton, New Jersey 08543, United States , Albany Molecular Research Inc , 21 Corporate Circle, Albany, New York 12203, United States , Bristol Myers-Squibb Research and Development , Princeton, New Jersey 08543, United States , Albany Molecular Research Inc , 21 Corporate Circle, Albany, New York 12203, United States , Bristol Myers-Squibb Research and Development , Princeton, New Jersey 08543, United States , Bristol Myers-Squibb Research and Development , Princeton, New Jersey 08543, United States , Albany Molecular Research Inc , 21 Corporate Circle, Albany, New York 12203, United States , Bristol Myers-Squibb Research and Development , Princeton, New Jersey 08543, United States , Bristol Myers-Squibb Research and Development , Princeton, New Jersey 08543, United States , Bristol Myers-Squibb Research and Development , Princeton, New Jersey 08543, United States , Bristol Myers-Squibb Research and Development , Princeton, New Jersey 08543, United States , Bristol Myers-Squibb Research and Development , Princeton, New Jersey 08543, United States , Bristol Myers-Squibb Research and Development , Princeton, New Jersey 08543, United States , Bristol Myers-Squibb Research and Development , Princeton, New Jersey 08543, United States , Bristol Myers-Squibb Research and Development , Princeton, New Jersey 08543, United States , Bristol Myers-Squibb Research and Development , Princeton, New Jersey 08543, United States

PubMed