43156-26-9Relevant articles and documents
New benzimidazole-2-urea derivates as tubulin inhibitors
Wang, Wenna,Kong, Dexin,Cheng, Huimin,Tan, Li,Zhang, Zhang,Zhuang, Xiaoxi,Long, Huoyou,Zhou, Yang,Xu, Yong,Yang, Xiaohong,Ding, Ke
, p. 4250 - 4253 (2014/09/29)
Emerging drug resistance and other drawbacks limit tubulin inhibitors' therapeutic applications and developing novel tubulin inhibitors still attracts intensive efforts. We describe the discovery and structure-activity relationship study of a series of benzimidazole-2-urea derivatives as novel β tubulin inhibitors. The representative compound 6o potently suppressed the proliferation of a panel of human cancer cells (NCI-H460, Colo205, K562, A431, HepG2, Hela, MDA-MB-435S) with IC50 values of 0.040, 0.050, 0.006, 0.026, 1.774, 0.452 and 0.052 μM, respectively. Compound 6o obviously inhibited NCI-H460 spindles formation and induced cell cycle arrest at G2/M phase at 0.10 μM. Computational study suggested that 6o interacts with β tubulin in a novel binding mode. Our results suggested that benzimidazole-2-urea derivatives might be promising tubulin inhibitors with novel binding mode for further development.
Synthesis and spectral properties of methyl 5-[(o-, m-, and p-r)- phenoxy]-2-benzimidazolecarbamate
Cortes,Anaya
, p. 745 - 748 (2007/10/03)
The preparation of eleven novel methyl 5-[(o-, m-, p-R)-phenoxy-2- benzimidazolecarbamates with possible pharmacological activity as anthelmintics is described. The structure of all products was corroborated by it, 1H-nmr, 13C-nmr and mass spectra.