[2.2.1]-Bicyclic sultams as potent androgen receptor antagonists

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 compound 25, which displayed robust pharmacodynamic effects in rats after oral dosing. (C) 2016 Elsevier Ltd. All rights reserved.