Synthesis and biological evaluation of benzamides and benzamidines as selective inhibitors of VEGFR tyrosine kinases

H Nakamura, Y Sasaki, M Uno, T Yoshikawa…

文献索引：Nakamura, Hiroyuki; Sasaki, Yusuke; Uno, Masaharu; Yoshikawa, Tomohiro; Asano, Toru; Ban, Hyun Seung; Fukazawa, Hidesuke; Shibuya, Masabumi; Uehara, Yoshimasa Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 19 p. 5127 - 5131

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被引用次数: 35

摘要

A series of benzamidines and benzamides was synthesized as selective inhibitors of vascular endothelial growth factor receptor (VEGFR) tyrosine kinases, and tested for inhibitory activity toward autophosphorylation by the enzyme assay. Selective inhibition of VEGFR-2 tyrosine kinase was observed in the salicylic amide 4e and the anthranilic amidine 5a, and their percent inhibitions of VEGFR-2 tyrosine kinase were 44–60% at a 10μM ...