O-Linked Triazolotriazines: Potent and Selective c-Met Inhibitors (pages 1276–1285)
Fang Chen, Ying Wang, Dr. Jing Ai, Zhengsheng Zhan, Yongcong Lv, Zhongjie Liang, Dr. Cheng Luo, Dr. Desheng Mei, Prof. Meiyu Geng and Prof. Wenhu Duan
Article first published online: 26 APR 2012 | DOI: 10.1002/cmdc.201200145
Highly selective c-Met inhibitor: c-Met is considered one of the most promising therapeutic targets for anticancer drug discovery. Herein we report a series of O-linked triazolotriazines that inhibit c-Met at sub-nanomolar concentrations. Compound 6 a exhibits high c-Met inhibitory potency in both enzymatic and cellular assays with great selectivity.