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