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

Terry V. Hughes; Stuart L. Emanuel; Amanda K. Beck; Steven K. Wetter; Peter J. Connolly; Prabha Karnachi; Michael Reuman; Jabed Seraj; Angel R. Fuentes-Pesquera; Robert H. Gruninger; Steven A. Middleton; Ronghui Lin; Jeremy M. Davis; David F.C. Moffat

doi:10.1016/j.bmcl.2007.04.021

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

Journal article

Peer reviewed

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

Terry V. Hughes, Stuart L. Emanuel, Amanda K. Beck, Steven K. Wetter, Peter J. Connolly, Prabha Karnachi, Michael Reuman, Jabed Seraj, Angel R. Fuentes-Pesquera, Robert H. Gruninger, …

Bioorganic & medicinal chemistry letters, Vol.17(12), pp.3266-3270

15/06/2007

DOI: https://doi.org/10.1016/j.bmcl.2007.04.021

PMID: 17481894

Abstract

2-Aminopyrimidines

Angiogenesis

Cancer

KDR

Kinase

Kinase inhibitor

VEGF-R2

A novel series of 4-aryl-5-cyano-2-aminopyrimidines 2 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. 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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Title: 4-Aryl-5-cyano-2-aminopyrimidines as VEGF-R2 inhibitors: Synthesis and biological evaluation
Creators - without role: Terry V. Hughes - Johnson & Johnson
Stuart L. Emanuel - Johnson & Johnson
Amanda K. Beck - Johnson & Johnson
Steven K. Wetter - Johnson & Johnson
Peter J. Connolly - Johnson & Johnson
Prabha Karnachi - Johnson & Johnson
Michael Reuman - Johnson & Johnson
Jabed Seraj - Johnson & Johnson
Angel R. Fuentes-Pesquera - Johnson & Johnson
Robert H. Gruninger - Johnson & Johnson
Steven A. Middleton - Johnson & Johnson
Ronghui Lin - Johnson & Johnson
Jeremy M. Davis - UCB Pharma
David F.C. Moffat - UCB Pharma, 216 Bath Road, Slough SL14EN, UK
Publication Details: Bioorganic & medicinal chemistry letters, Vol.17(12), pp.3266-3270
Publisher: Elsevier Ltd
Identifiers: 9941871908331
Academic Unit: King Abdullah University of Science & Technology
Language: English
Resource Type: Journal article