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Citation: Li Hongxia, Qian Yumei, Wang Haichao, Shan Lingling. Design, Syntheses and Biological Evaluations of 2-Thiol Benzimidazole Derivatives as Potential Anticancer Agent[J]. Chemistry, ;2019, 82(10): 909-916. shu

Design, Syntheses and Biological Evaluations of 2-Thiol Benzimidazole Derivatives as Potential Anticancer Agent

School of Life and Food Engineering, Suzhou University, Suzhou Anhui 234000

Received Date: 22 April 2019
Accepted Date: 15 July 2019

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In order to find novel benzimidazole derivatives having potent bioactivities, a series of 2-thiol benzimidazole derivatives (4a~4q) were designed and synthesized using bromacetic acid as starting material. Their cell antiproliferative activities against human cervical cancer cell line (Hela), human breast cancer cells (MCF-7), human hepatoma cells (HepG2) and human non-small cell lung cancer cell lines cells (A549) were estimated in vitro via thiazolyl blue tetrazolium bromide (MTT) assay method. The results showed that most target compounds exhibit moderate antitumor activities, especially the compound 2-((1H-benzo[d]imidazol-2-yl)thio)-1-(4-benzhydrylpiperazin-1-yl)ethan-1-one (4l) has stronger inhibitory activity against HepG2 cell lines with the IC₅₀ value of 12.62±0.78μmol/L, which is close to the control Gefitinib (11.72±0.38μmol/L). Moreover, the structure-activity relationship (SAR) of the derivatives was discussed by molecular studies.
- Benzimidazole derivatives,
- Anti-tumor activity,
- EGFR inhibitors
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