中国药科大学学报2017，Vol.48Issue(6)：670-674,5.DOI:10.11665/j.issn.1000-5048.20170606
吡啶类IRAK4抑制剂的设计、合成及生物活性评价
Design, synthesis and biological evaluation of pyridine-based IRAK4 inhibitors
摘要
Abstract
Based on the known IRAK4 inhibitors MK-32 and AU-5,we designed and synthesized 12 pyridine-based target compounds by adopting open-ring and hybrid strategies,and combining molecular docking technology.The bioassays determined by radioisotope labeling demonstrated that the target compounds displayed good inhibitory activity against IRAK4.Among them,the IC50 value of 5 compounds was less than 1 μmol/L,suggesting that these compounds may be candidates for further investigation.关键词
IRAK4抑制剂/设计/合成/生物活性Key words
IRAK4 inhibitor/design/synthesis/biological evaluation分类
医药卫生引用本文复制引用
朱宝,金双龙,郭毅,李月珍,张奕华,赖宜生..吡啶类IRAK4抑制剂的设计、合成及生物活性评价[J].中国药科大学学报,2017,48(6):670-674,5.基金项目
国家自然科学基金资助项目(No.21472244)This work was supported by the National Natural Science Foundation of China (No.21472244) （No.21472244）
