56073-96-2Relevant articles and documents
Discovery of novel benzimidazoles as potent inhibitors of TIE-2 and VEGFR-2 tyrosine kinase receptors
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
, p. 4453 - 4470 (2008/02/13)
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 urea moiety when the benzimidazole-urea compounds were bound to the VEGFR-2 enzyme. The left side phenyl ring (segment A) occupies the backpocket where a 3-hydrophobic substituent was favored for TIE-2 activity.
Chemical compounds
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, (2008/06/13)
Benzimidazole derivatives, which are useful as TIE-2 and/or VEGFR2 inhibitors are described herein. The described invention also includes methods of making such benzimidazole derivatives as well as methods of using the same in the treatment of hyperproliferative diseases.
Bis-arylsulfonamide derivatives of 2-amino-5(6)-(4-aminophenylthio)benzimidazole
Pilyugin,Mikhailyuk,Kosareva
, p. 1782 - 1789 (2007/10/03)
Three different procedures have been developed for the preparation of bis-arylsulfonamide derivatives of 2-amino-5(6)-(4-aminophenylthio)benzimidazole, and biological activity of the products have been studied.
Syntheses and Anthelmintic Activity of 2-Substituted 5(6)-Arylthio- and 5(6)-Arylsulphono-benzimidazoles
Abuzar, Syed,Rao, K. V. B.,Sharma, Satyavan,Gupta, Suman,Katiyar, J. C.
, p. 178 - 181 (2007/10/02)
A series of 2-substituted 5(6)-arylthio- and 5(6)-arylsulphono-benzimidazoles (7-32) have been prepared and tested for their anthelmintic activity.Among the compounds tested against Hymenolepis nana infection in rats and mice and Ancylostoma ceylanicum in