Design, synthesis and biological evaluation of pyridine-based IRAK4 inhibitors
10.11665/j.issn.1000-5048.20170606
- VernacularTitle:吡啶类IRAK4抑制剂的设计、合成及生物活性评价
- Author:
Bao ZHU
1
;
Shuanglong JIN
;
Yi GUO
;
Yuezhen LI
;
Yihua ZHANG
;
Yisheng LAI
Author Information
1. 中国药科大学新药研究中心
- Keywords:
IRAK4 inhibitor;
design;
synthesis;
biological evaluation
- From:
Journal of China Pharmaceutical University
2017;48(6):670-674
- CountryChina
- Language:Chinese
-
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.
