de novo design and synthesis of N-benzylanilines as new candidates for VEGFR tyrosine kinase inhibitors |
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| Authors: | Uno Masaharu Ban Hyun Seung Nabeyama Wataru Nakamura Hiroyuki |
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| Institution: | Department of Chemistry, Faculty of Science, Gakushuin University, 1-5-1 Mejiro, Toshima-ku, Tokyo 171-8588, Japan. |
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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 showed the most potent inhibitory activity toward VEGFR-2 (KDR) tyrosine kinase and its IC(50) value was 0.57 microM. |
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