4-Aryl-5-cyano-2-aminopyrimidines as VEGF-R2 inhibitors: synthesis and biological evaluation

…, J Seraj, AR Fuentes-Pesquera, RH Gruninger…

文献索引：Hughes, Terry V.; Emanuel, Stuart L.; Beck, Amanda K.; Wetter, Steven K.; Connolly, Peter J.; Karnachi, Prabha; Reuman, Michael; Seraj, Jabed; Fuentes-Pesquera, Angel R.; Gruninger, Robert H.; Middleton, Steven A.; Lin, Ronghui; Davis, Jeremy M.; Moffat, David F.C. Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 12 p. 3266 - 3270

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被引用次数: 36

摘要

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.