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

, : Identification of potent and selective VEGFR receptor tyrosine kinase inhibitors having new amide isostere headgroups. Bioorganic & Medicinal Chemistry Letters 20(3): 848-852

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.


PMID: 20071170

DOI: 10.1016/j.bmcl.2009.12.099

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