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4-Aryl-5-cyano-2-aminopyrimidines as VEGF-R2 inhibitors: synthesis and biological evaluation |
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| Authors: | 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 |
| Institution: | Johnson & Johnson Pharmaceutical Research and Development, L.L.C, PO Box 300, 1000 Route 202, Raritan, NJ 08869, USA. hughe007@hotmail.com |
| 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. |
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