(1,2,3-Triazol-4-yl)benzenamines: Synthesis and activity against VEGF receptors 1 and 2

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 (TM) in both HTRF enzymatic and cellular assays. (C) 2009 Elsevier Ltd. All rights reserved.