Structure-based optimization of aminopyridines as PKCθ inhibitors.
Bioorganic & Medicinal Chemistry Letters(2012)
摘要
The identification of a novel series of PKCθ inhibitors and subsequent optimization using docking based on a crystal structure of PKCθ is described. SAR was rapidly generated around an amino pyridine-ketone hit; (6-aminopyridin-2-yl)(2-aminopyridin-3-yl)methanone 2 leading to compound 21 which significantly inhibits production of IL-2 in a mouse SEB-IL2 model.
更多查看译文
关键词
PKCθ,Kinase,SEB-IL2,Aminopyridine,T cell receptor
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