title: Hetaryl imidazoles: a novel dual inhibitors of VEGF receptors I and II.
abstract: A novel potent derivatives of hetaryl imidazoles were described as inhibitors of vascular endothelial growth factor receptor II (VEGFR-2). Several compounds display VEGFR-2 inhibitory activity reaching IC(50)<100 nM in both enzymatic and cellular assays. The compounds also inhibit the related tyrosine kinase, VEGFR-1. By controlling the substitution pattern on the 5-carboxamido functionality, both dual and specific VEGFR-2 thiazoles were identified.
authors.affiliation: Small Molecule Drug Discovery, Chemical Diversity, Inc., 11558 Sorrento Valley Road, San Diego, CA 92121, USA. ask@chemdiv.com
authors.forename: Alexander S
authors.initials: AS
authors.lastname: Kiselyov
authors.forename: Marina
authors.initials: M
authors.lastname: Semenova
authors.forename: Victor V
authors.initials: VV
authors.lastname: Semenov
authors.forename: Evgueni
authors.initials: E
authors.lastname: Piatnitski
authors.forename: Shawn
authors.initials: S
authors.lastname: Ouyang
mesh_terms: D007093:Imidazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D040281:Vascular Endothelial Growth Factor Receptor-1 / Q000037:antagonists & inhibitors* / Q000378:metabolism; D040301:Vascular Endothelial Growth Factor Receptor-2 / Q000037:antagonists & inhibitors* / Q000378:metabolism
chemical_list: D007093:Imidazoles; D040281:Vascular Endothelial Growth Factor Receptor-1; D040301:Vascular Endothelial Growth Factor Receptor-2