2-((1H-Azol-1-yl)methyl)-N-arylbenzamides: novel dual inhibitors of VEGFR-1/2 kinases.

Article Details

Citation

Kiselyov AS, Semenova M, Semenov VV, Piatnitski E

2-((1H-Azol-1-yl)methyl)-N-arylbenzamides: novel dual inhibitors of VEGFR-1/2 kinases.

Bioorg Med Chem Lett. 2006 Mar 15;16(6):1726-30. Epub 2005 Dec 20.

PubMed ID
16364640 [ View in PubMed
]
Abstract

Novel potent derivatives of (azol-1-yl)methyl-N-arylbenzamides with improved solubility (>3mM) are described as ATP-competitive inhibitors of vascular endothelial growth factor receptor 2 (VEGFR-2). Many compounds display VEGFR-2 inhibitory activity reaching IC(50)<100 nM in the enzymatic assay. The compounds also inhibit the related tyrosine kinase, VEGFR-1, with similar potencies. Several compounds containing bulky lipophilic substituents at the benzamide pharmacophore yielded 10- to 17-fold selectivity for the VEGFR-2 versus VEGFR-1 kinase.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
VatalanibVascular endothelial growth factor receptor 1IC 50 (nM)140N/AN/ADetails
VatalanibVascular endothelial growth factor receptor 2IC 50 (nM)54N/AN/ADetails