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Bioorg Med Chem Lett. 2010 Feb 1;20(3):848-52. doi: 10.1016/j.bmcl.2009.12.099. Epub 2010 Jan 4.

Identification of potent and selective VEGFR receptor tyrosine kinase inhibitors having new amide isostere headgroups.

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  • 1Department of Medicinal Chemistry, MethylGene Inc, 7220 rue Frederick-Banting, MontrĂ©al, QC, Canada H4S 2A1.


A novel series of malonamide-type dual VEGFR2/c-Met inhibitors in which one of the amide bonds was replaced by an amide isostere-a trifluoroethylamine unit, was designed, synthesized, and evaluated for their enzymatic and cellular inhibition of VEGFR2 and c-Met enzymes. Optimization of these molecular entities resulted in identification of potent and selective inhibitors of VEGFR2 enzyme.

Copyright (c) 2010. Published by Elsevier Ltd.

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