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Issue 6, 2008
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de novo Design and synthesis of N-benzylanilines as new candidates for VEGFR tyrosinekinase inhibitors

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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

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Publication details

The article was received on 02 Jan 2008, accepted on 24 Jan 2008 and first published on 11 Feb 2008


Article type: Communication
DOI: 10.1039/B719959G
Citation: Org. Biomol. Chem., 2008,6, 979-981
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    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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