2-((1H-Azol-1-yl)methyl)-N-arylbenzamides: novel dual inhibitors of VEGFR-1/2 kinases.
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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
Drug Target Property Measurement pH Temperature (°C) Vatalanib Vascular endothelial growth factor receptor 1 IC 50 (nM) 140 N/A N/A Details Vatalanib Vascular endothelial growth factor receptor 2 IC 50 (nM) 54 N/A N/A Details