Issue 22, 2014

Design and synthesis of 3,3′-biscoumarin-based c-Met inhibitors

Abstract

A library of biscoumarin-based c-Met inhibitors was synthesized, based on optimization of 3,3′-biscoumarin hit 3, which was identified as a non-ATP competitive inhibitor of c-Met from a diverse library of coumarin derivatives. Among these compounds, 38 and 40 not only showed potent enzyme activities with IC50 values of 107 nM and 30 nM, respectively, but also inhibited c-Met phosphorylation in BaF3/TPR-Met and EBC-1 cells.

Graphical abstract: Design and synthesis of 3,3′-biscoumarin-based c-Met inhibitors

Supplementary files

Article information

Article type
Paper
Submitted
17 Feb 2014
Accepted
03 Apr 2014
First published
03 Apr 2014

Org. Biomol. Chem., 2014,12, 3721-3734

Author version available

Design and synthesis of 3,3′-biscoumarin-based c-Met inhibitors

J. Xu, J. Ai, S. Liu, X. Peng, L. Yu, M. Geng and F. Nan, Org. Biomol. Chem., 2014, 12, 3721 DOI: 10.1039/C4OB00364K

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