Discovery of BMS-641988, a Novel Androgen Receptor Antagonist for the Treatment of Prostate Cancer
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- 作者：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
- 刊名：ACS Medicinal Chemistry Letters
- 出版年：2015
- 出版时间：August 13, 2015
- 年：2015
- 卷：6
- 期：8
- 页码：908-912
- 全文大小：310K
- ISSN：1948-5875
文摘
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.