title: 1H-1,2,4-triazol-3-yl-anilines: novel potent inhibitors of vascular endothelial growth factor receptors 1 and 2.
abstract: 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.
authors.affiliation: ChemDiv Inc., 6605 Nancy Ridge Drive, San Diego, CA 92121, USA. ask@chemdiv.com
authors.forename: Alexander S
authors.initials: AS
authors.lastname: Kiselyov
authors.forename: Evgueni
authors.initials: E
authors.lastname: Piatnitski
authors.forename: Daniel
authors.initials: D
authors.lastname: Milligan
authors.forename: Xiaohu
authors.initials: X
authors.lastname: Ouyang
mesh_terms: 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*
chemical_list: D000814:Aniline Compounds; D014230:Triazoles; D040262:Receptors, Vascular Endothelial Growth Factor; C023650:aniline