title: Arylphthalazines: identification of a new phthalazine chemotype as inhibitors of VEGFR kinase.
abstract: A novel class of 4-arylamino-phthalazin-1-yl-benzamides is described as inhibitors of vascular endothelial growth factor receptor II (VEGFR-2). Several compounds display potent VEGFR-2 inhibitory activity with an IC50 as low as 0.078 microM in an HTRF enzymatic assay. These compounds are relatively selective against a small kinase panel.
authors.affiliation: Department of Chemistry, ImClone Systems, 710 Parkside Avenue, Suite 2, Brooklyn, NY 11226, USA.
authors.forename: Evgueni L
authors.initials: EL
authors.lastname: Piatnitski
authors.forename: Matthew A J
authors.initials: MA
authors.lastname: Duncton
authors.forename: Alexander S
authors.initials: AS
authors.lastname: Kiselyov
authors.forename: Reeti
authors.initials: R
authors.lastname: Katoch-Rouse
authors.forename: Dan
authors.initials: D
authors.lastname: Sherman
authors.forename: Daniel L
authors.initials: DL
authors.lastname: Milligan
authors.forename: Chris
authors.initials: C
authors.lastname: Balagtas
authors.forename: Wai C
authors.initials: WC
authors.lastname: Wong
authors.forename: Joel
authors.initials: J
authors.lastname: Kawakami
authors.forename: Jacqueline F
authors.initials: JF
authors.lastname: Doody
mesh_terms: D020533:Angiogenesis Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D020128:Inhibitory Concentration 50; D010793:Phthalazines / Q000138:chemical synthesis* / Q000494:pharmacology; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D040262:Receptors, Vascular Endothelial Growth Factor / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D040281:Vascular Endothelial Growth Factor Receptor-1 / Q000037:antagonists & inhibitors; D040301:Vascular Endothelial Growth Factor Receptor-2 / Q000037:antagonists & inhibitors
chemical_list: D020533:Angiogenesis Inhibitors; D010793:Phthalazines; D047428:Protein Kinase Inhibitors; C043388:phthalazine; D040262:Receptors, Vascular Endothelial Growth Factor; D040281:Vascular Endothelial Growth Factor Receptor-1; D040301:Vascular Endothelial Growth Factor Receptor-2