Issue 6, 2008

de novo Design and synthesis of N-benzylanilines as new candidates for VEGFR tyrosinekinase inhibitors

Abstract

N-Benzylanilines were designed and synthesized as vascular endothelial growth factor (VEGF)-2 inhibitors using de novo drug design systems based on the X-ray structure of VEGFR-2 kinase domain. Among compounds synthesized, compound 3 showed the most potent inhibitory activity toward VEGFR-2 (KDR) tyrosinekinase and its IC50 value was 0.57 µM.

Graphical abstract: de novo Design and synthesis of N-benzylanilines as new candidates for VEGFR tyrosinekinase inhibitors

Supplementary files

Article information

Article type
Communication
Submitted
02 Jan 2008
Accepted
24 Jan 2008
First published
11 Feb 2008

Org. Biomol. Chem., 2008,6, 979-981

de novo Design and synthesis of N-benzylanilines as new candidates for VEGFR tyrosinekinase inhibitors

M. Uno, H. S. Ban, W. Nabeyama and H. Nakamura, Org. Biomol. Chem., 2008, 6, 979 DOI: 10.1039/B719959G

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