CuI-mediated synthesis of 1-aryl-5,6,7-trimethoxybenzimidazoles as potent antitubulin agents

Cong Min Peng, Shih Wei Wang, Yi Lin Hwang, Wen Chun Sun, Li Pin Chiu, Yi Ting Liu, Yu Wei Lai, Hsueh Yun Lee

Research output: Contribution to journalArticlepeer-review


In situ CuI-mediated cyclization methodology helped yield benzimidazoles with different substitution manner, such as 1,2-diarylbenzimidazoles (4 and 5) and 1-arylbenzimidazoles (6-15). The result of structure-activity relationship (SAR) study confirmed the significance of the 5,6,7-trimethoxybenzimidazole moiety, and the representative derivatives (8-10) exhibited marked antiproliferative activity against A549, HCT-116, and PC-3 cells; in addition, they are able to inhibit the polymerization of tubulin. Among them, compound 10 inhibited the growth of A549, HCT-116, and PC-3 cells with a mean IC50 value of 0.07 μM, and its IC50 value of tubulin polymerization is 0.26 μM.

Original languageEnglish
Pages (from-to)13169-13176
Number of pages8
JournalRSC Advances
Issue number19
Publication statusPublished - Apr 28 2023

ASJC Scopus subject areas

  • Chemistry(all)
  • Chemical Engineering(all)


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