title: Discovery of AZD2932, a new Quinazoline Ether Inhibitor with high affinity for VEGFR-2 and PDGFR tyrosine kinases.
abstract: A new series of Quinazoline Ether Inhibitor which potently inhibits VEGFR-2 and PDGFR tyrosine kinases is described here. In vitro, pharmacokinetics and in vivo evaluations led to the selection of AZD2932.
authors.affiliation: AstraZeneca, Centre de Recherches, B.P. 1050, 51689 Reims Cedex 2, France. patrick.ple@astrazeneca.com
authors.forename: Patrick A
authors.initials: PA
authors.lastname: Plé
authors.forename: Frédéric
authors.initials: F
authors.lastname: Jung
authors.forename: Sue
authors.initials: S
authors.lastname: Ashton
authors.forename: Laurent
authors.initials: L
authors.lastname: Hennequin
authors.forename: Romuald
authors.initials: R
authors.lastname: Laine
authors.forename: Rémy
authors.initials: R
authors.lastname: Morgentin
authors.forename: Georges
authors.initials: G
authors.lastname: Pasquet
authors.forename: Sian
authors.initials: S
authors.lastname: Taylor
mesh_terms: D000465:Algorithms; D000818:Animals; D002626:Chemistry, Pharmaceutical / Q000379:methods; D004285:Dogs; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology; D004987:Ethers / Q000138:chemical synthesis* / Q000494:pharmacology*; D005260:Female; D006801:Humans; D020128:Inhibitory Concentration 50; D008297:Male; D008956:Models, Chemical; D010766:Phosphorylation; D011799:Quinazolines / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats; D020797:Receptor, Platelet-Derived Growth Factor beta / Q000037:antagonists & inhibitors*; D040301:Vascular Endothelial Growth Factor Receptor-2 / Q000037:antagonists & inhibitors*
chemical_list: C573778:AZD2932; D004791:Enzyme Inhibitors; D004987:Ethers; D011799:Quinazolines; D020797:Receptor, Platelet-Derived Growth Factor beta; D040301:Vascular Endothelial Growth Factor Receptor-2