Discovery of novel benzimidazoles as potent inhibitors of TIE-2 and VEGFR-2 tyrosine kinase receptors

…, RI West, M Shibahara, H Toyoda, L Wang…

文献索引：Hasegawa, Masaichi; Nishigaki, Naohiko; Washio, Yoshiaki; Kano, Kazuya; Harris, Philip A.; Sato, Hideyuki; Mori, Ichiro; West, Rob I.; Shibahara, Megumi; Toyoda, Hiroko; Wang, Liping; Nolte, Robert T.; Veal, James M.; Cheung, Mui Journal of Medicinal Chemistry, 2007 , vol. 50, # 18 p. 4453 - 4470

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被引用次数: 112

摘要

We herein disclose a novel chemical series of benzimidazole-ureas as inhibitors of VEGFR- 2 and TIE-2 kinase receptors, both of which are implicated in angiogenesis. Structure-activity relationship (SAR) studies elucidated a critical role for the N1 nitrogen of both the benzimidazole (segment E) and urea (segment B) moieties. The SAR results were also supported by the X-ray crystallographic elucidation of the role of the N1 nitrogen and the ...