title: 4-Aryl-5-cyano-2-aminopyrimidines as VEGF-R2 inhibitors: synthesis and biological evaluation.
abstract: A novel series of 4-aryl-5-cyano-2-aminopyrimidines were synthesized and found to have potent VEGF-R2 kinase inhibitory activity. Structure-activity relationships were investigated and compound 14a was shown to be efficacious in a mouse model of corneal neovascularization.
authors.affiliation: Johnson & Johnson Pharmaceutical Research and Development, L.L.C, PO Box 300, 1000 Route 202, Raritan, NJ 08869, USA. hughe007@hotmail.com
authors.forename: Terry V
authors.initials: TV
authors.lastname: Hughes
authors.forename: Stuart L
authors.initials: SL
authors.lastname: Emanuel
authors.forename: Amanda K
authors.initials: AK
authors.lastname: Beck
authors.forename: Steven K
authors.initials: SK
authors.lastname: Wetter
authors.forename: Peter J
authors.initials: PJ
authors.lastname: Connolly
authors.forename: Prabha
authors.initials: P
authors.lastname: Karnachi
authors.forename: Michael
authors.initials: M
authors.lastname: Reuman
authors.forename: Jabed
authors.initials: J
authors.lastname: Seraj
authors.forename: Angel R
authors.initials: AR
authors.lastname: Fuentes-Pesquera
authors.forename: Robert H
authors.initials: RH
authors.lastname: Gruninger
authors.forename: Steven A
authors.initials: SA
authors.lastname: Middleton
authors.forename: Ronghui
authors.initials: R
authors.lastname: Lin
authors.forename: Jeremy M
authors.initials: JM
authors.lastname: Davis
authors.forename: David F C
authors.initials: DF
authors.lastname: Moffat
mesh_terms: D000818:Animals; D016510:Corneal Neovascularization / Q000188:drug therapy* / Q000473:pathology; D004195:Disease Models, Animal; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology / Q000627:therapeutic use*; D051379:Mice; D011743:Pyrimidines / Q000138:chemical synthesis / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D040301:Vascular Endothelial Growth Factor Receptor-2 / Q000037:antagonists & inhibitors*
chemical_list: D004791:Enzyme Inhibitors; D011743:Pyrimidines; D040301:Vascular Endothelial Growth Factor Receptor-2