Hetaryl imidazoles: A novel dual inhibitors of VEGF receptors I and II

A novel potent derivatives of hetaryl imidazoles were described as inhibitors of vascular endothelial growth factor receptor II (VEGFR-2). Several compounds display VEGFR-2 inhibitory activity reaching IC50 < 100 nM in both enzymatic and cellular assays. The compounds also inhibit the related tyrosine kinase, VEGFR-1. By controlling the substitution pattern on the 5-carboxamido functionality, both dual and specific VEGFR-2 thiazoles were identified.

Graphical abstractNovel potent derivatives of hetaryl imidazoles are described as inhibitors of vascular endothelial growth factor receptor II (VEGFR-2). Many compounds display VEGFR-2 inhibitory activity reaching IC50 < 100 nM in both enzymatic and cell-based assays. The compounds also inhibit the related tyrosine kinase, VEGFR-1, with similar potencies. By controlling the substitution pattern on the 5-carboxamido pharmacophore, both dual and specific VEGFR-2 thiazoles were identified.Figure optionsDownload full-size imageDownload as PowerPoint slide