期刊论文

Huang, Wei

英文

Bioorganic & Medicinal Chemistry Letters

0960-894X

2014

24

15

3351-3355

10.1016/j.bmcl.2014.05.097

This work was supported by the National Natural Science Foundation of China (No. 21272086 ). The authors would like to thank Prof. Guangfu Yang of Central China Normal University for conducting molecular stimulation.

本校为第一且通讯机构

The high incidence of MET oncogene activation in human malignancies has prompted researchers to develop MET inhibitors. As part of our efforts to developing effective and safe therapeutic agents against MET-dependent tumors, a pyridone-based class II MET inhibitor, namely, 1-(4-((2-amino-3-iodopyridin-4- yl)-oxy)-3-fluorophenyl)-N-(4-fluorobenzyl)-4-methoxy-6-oxo-1, 6-dihydropyridine-3-carboxamide (3s), was identified. Knowledge of the binding mode of class II MET inhibitors led to the design of new inhibitors that utilize 2-pyridone to conform...