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 Vatalanib and Vandetanib in both homogenous time-resolved fluorescence enzymatic and cellular assays. Several active molecules feature high intrinsic permeability (>30 x 10(-5) cm/min) across Caco-2 cell monolayer.
Kiselyov
Alexander S
AS
ChemDiv Inc., 6605 Nancy Ridge Drive, San Diego, CA 92121, USA. ask@chemdiv.com
Piatnitski
Evgueni
E
Milligan
Daniel
D
Ouyang
Xiaohu
X
D000814:Aniline Compounds / Q000737:chemistry*; D002478:Cells, Cultured; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D040262:Receptors, Vascular Endothelial Growth Factor / Q000037:antagonists & inhibitors*; D021241:Spectrometry, Mass, Electrospray Ionization; D014230:Triazoles / Q000737:chemistry / Q000494:pharmacology*
D000814:Aniline Compounds; D014230:Triazoles; D040262:Receptors, Vascular Endothelial Growth Factor; C023650:aniline