These authors contributed equally to this work.
O-Linked Triazolotriazines: Potent and Selective c-Met Inhibitors
Version of Record online: 26 APR 2012
Copyright © 2012 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim
Volume 7, Issue 7, pages 1276–1285, July 2012
How to Cite
Chen, F., Wang, Y., Ai, J., Zhan, Z., Lv, Y., Liang, Z., Luo, C., Mei, D., Geng, M. and Duan, W. (2012), O-Linked Triazolotriazines: Potent and Selective c-Met Inhibitors. ChemMedChem, 7: 1276–1285. doi: 10.1002/cmdc.201200145
- Issue online: 25 JUN 2012
- Version of Record online: 26 APR 2012
- Manuscript Revised: 14 APR 2012
- Manuscript Received: 16 MAR 2012
- National Natural Science Foundation. Grant Numbers: 81102461, 81021062, 90813034
- National Science & Technology Major Project. Grant Numbers: 2012ZX09301-001-007, 2012ZX09103101-024
- Shanghai Science and Technology Commission. Grant Number: 11431921100
- tyrosine kinase
The HGF/c-Met signaling pathway mediates a variety of important biological activities, but dysregulation of the pathway is also closely associated with poor prognosis in a wide range of human cancers. c-Met is considered to be among the most promising therapeutic targets for anticancer drug discovery. Herein we report the discovery of a series of O-linked triazolotriazines that show sub-nanomolar inhibition of c-Met activity. Among these new compounds, 6 a exhibits high c-Met inhibitory potency in both enzymatic and cellular assays with great selectivity.