[2.2.1]-Bicyclic sultams as potent androgen receptor antagonists.

Weifang Shan,Aaron Balog,Andrew Nation,Xiao Zhu,Jing Chen,Mary Ellen Cvijic,Jieping Geng,Cheryl A Rizzo,Thomas Spires,Ricardo M Attar,Mary Obermeier,Sarah Traeger,Jun Dai,Yingru Zhang,Michael Galella,George Trainor,Gregory D Vite,Ashvinikumar V Gavai

Bioorganic & Medicinal Chemistry Letters（2016）

引用 10|浏览77

暂无评分

摘要

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.

查看译文

关键词

Cancer,Nuclear hormone receptor,Androgen receptor antagonist,Pharmacokinetics and pharmacodynamics

AI 理解论文

溯源树

样例

生成溯源树，研究论文发展脉络

Chat Paper

正在生成论文摘要