[2.2.1]-Bicyclic sultams as potent androgen receptor antagonists. Issue 23 (1st December 2016)

• Record Type: Journal Article
• Authors: Shan, Weifang; Balog, Aaron; Nation, Andrew; Zhu, Xiao; Chen, Jing; Cvijic, Mary Ellen; Geng, Jieping; Rizzo, Cheryl A.; Spires, Thomas; Attar, Ricardo M.; Obermeier, Mary; Traeger, Sarah; Dai, Jun; Zhang, Yingru; Galella, Michael; Trainor, George; Vite, Gregory D.; Gavai, Ashvinikumar V.
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 26:Issue 23(2016)
• Page Start: 5707
• Page End: 5711
• Publication Date: 2016-12-01
• Subjects: Cancer -- Nuclear hormone receptor -- Androgen receptor antagonist -- Pharmacokinetics and pharmacodynamics; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2016.10.059
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: This letter describes the discovery, synthesis, SAR, and biological activity of [2.2.1]-bicyclic sultams as potent antagonists of the androgen receptor. Optimization of the series led to the identification of compound25, which displayed robust pharmacodynamic effects in rats after oral dosing. Abstract: This letter describes the discovery, synthesis, SAR, and biological activity of [2.2.1]-bicyclic sultams as potent antagonists of the androgen receptor. Optimization of the series led to the identification of compound25, which displayed robust pharmacodynamic effects in rats after oral dosing.