2. Academic Validation
  3. New benzimidazole-2-urea derivates as tubulin inhibitors

New benzimidazole-2-urea derivates as tubulin inhibitors

  • Bioorg Med Chem Lett. 2014 Sep 1;24(17):4250-3. doi: 10.1016/j.bmcl.2014.07.035.
Wenna Wang 1,  Dexin Kong 1,  Huimin Cheng 2,  Li Tan 2,  Zhang Zhang 2,  Xiaoxi Zhuang 2,  Huoyou Long 2,  Yang Zhou 2,  Yong Xu 2,  Xiaohong Yang 3,  Ke Ding 4
Affiliations

Affiliations

  • 1 College of Pharmacy, Jilin University, Changchun 130021, China.
  • 2 Institute of Chemical Biology, Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences, #190 Kaiyuan Avenue, Guangzhou 510530, China.
  • 3 College of Pharmacy, Jilin University, Changchun 130021, China. Electronic address: xiaohongyang88@126.com.
  • 4 Institute of Chemical Biology, Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences, #190 Kaiyuan Avenue, Guangzhou 510530, China. Electronic address: ding_ke@gibh.ac.cn.
PMID: 25091926 DOI: 10.1016/j.bmcl.2014.07.035
Abstract

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.

Keywords

Ant-cancer; Benzimidazole-2-urea derivates; Cell cycle arrest; Microtubule; Tubulin inhibitors.

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