(1,2,3-Triazol-4-yl)benzenamines: synthesis and activity against VEGF receptors 1 and 2.
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Kiselyov AS, Semenova M, Semenov VV
(1,2,3-Triazol-4-yl)benzenamines: synthesis and activity against VEGF receptors 1 and 2.
Bioorg Med Chem Lett. 2009 Mar 1;19(5):1344-8. doi: 10.1016/j.bmcl.2009.01.046. Epub 2009 Jan 20.
- PubMed ID
- 19188066 [ View in PubMed]
- Abstract
Derivatives of (1,2,3-triazol-4-yl)benzenamines are described as potent and ATP-competitive inhibitors of vascular endothelial growth factor receptors I and II (VEGFR-1/2). A number of compounds exhibited VEGFR-2 and VEGFR-1 inhibitory activity comparable to that of Vatalanib in both HTRF enzymatic and cellular assays.
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 1 IC 50 (nM) 110 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 Vatalanib Vascular endothelial growth factor receptor 2 IC 50 (nM) 42 N/A N/A Details Vatalanib Vascular endothelial growth factor receptor 2 IC 50 (nM) 16 N/A N/A Details