Issue 6, 2008
From the journal:

Organic & Biomolecular Chemistry

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

Masaharu Uno,a   Hyun Seung Ban,a   Wataru Nabeyamaa  and  Hiroyuki Nakamura*a  

* Corresponding authors

a Department of Chemistry, Faculty of Science, Gakushuin University, 1-5-1 Mejiro, Toshima-ku, Tokyo 171-8588, Japan
E-mail: hiroyuki.nakamura@gakushuin.ac.jp
Fax: (+81) (0)3 5992 1029
Tel: (+81) (0)3 3986 0221

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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Article information

DOI
https://doi.org/10.1039/B719959G
Article type
Communication
Submitted
02 Jan 2008
Accepted
24 Jan 2008
First published
11 Feb 2008

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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