Evgueni Piatnitski

1-(Azolyl)-4-(aryl)-phthalazines: novel potent inhibitors of VEGF receptors I and II.

Novel potent derivatives of phthalazine are described as an adenosine triphosphate‐competitive inhibitors of vascular endothelial growth factor receptors I and II. A number of compounds display vascular endothelial growth factor receptor II inhibitory activity reaching that of VatalanibTMA (IC50: <50 nm) in an homogenous time‐resolved fluorescence enzymatic assay.

1H-1,2,4-triazol-3-yl-anilines: novel potent inhibitors of vascular endothelial growth factor receptors 1 and 2.

Novel derivatives of 1,2,4‐triazoles are described as potent ATP‐competitive inhibitors of vascular endothelial growth factor receptors I and II (VEGFR‐1/2). A number of compounds display VEGFR‐2 inhibitory activity comparable to that of VatalanibTM and VandetanibTM in both homogenous time‐resolved fluorescence enzymatic and cellular assays. Several active molecules feature high intrinsic permeability (>30 × 10−5 cm/min) across Caco‐2 cell monolayer.