Hetaryl imidazoles: a novel dual inhibitors of VEGF receptors I and II.
Article Details
- CitationCopy to clipboard
Kiselyov AS, Semenova M, Semenov VV, Piatnitski E, Ouyang S
Hetaryl imidazoles: a novel dual inhibitors of VEGF receptors I and II.
Bioorg Med Chem Lett. 2006 Mar 1;16(5):1440-4.
- PubMed ID
- 16321531 [ View in PubMed]
- Abstract
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 IC(50)<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.
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 Vatalanib Vascular endothelial growth factor receptor 2 IC 50 (nM) 21 N/A N/A Details