Novel Benzimidazole Derivatives: Cytotoxic and Apoptotic Properties on Lung Cancer Cell Line

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Author(s): Leyla Yurttas*, Gulsen Akalin Ciftci, Mehmet Onur Aksoy, Seref Demirayak.

Journal Name: Letters in Drug Design & Discovery

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Background: Benzimidazole derivatives are privileged molecules known with wide variety of biological activity. In medicinal chemistry, due to the ring’s structural similarity to nucleotides its derivatives were investigated as new chemotheraupeutic agents. Our research group have been studying about 1,2-disubstituted benzimidazoles including thiocarbamoyl group and their potential anticancer activity. Based on previous findings, we have synthesized novel 1-[2-(4-substituted phenyl-2-oxoethyl)]-2-[(2/3/4-substituted phenylpiperidin-1- yl)thiocarbamoyl]benzimidazole derivatives (3a-o).

Methods: The obtained fifteen derivatives were studied on A549 adenocarcinomic human alveolar basal epithelial cell line and mouse L929 fibroblastic cell line to determine their cytotoxic activity. These compounds were also investigated to identify their apoptotic properties.

Results: The structures of the compounds based on three different groups, they differ from each other with the phenyl substituents bonded to piperazine ring. All of the compounds showed remarkable antitumor activity, but first five compounds bearing non-substituted phenyl moiety exhibited selective cytotoxicity when compared potencies to normal cell line.

Conclusion: Compounds 3j, 3m and 3n were identified as the most apoptotic derivatives, however compounds 3e and 3h provoked apoptosis with the percentages of 10.6 and 10.9 % and selective cytotoxicity.

Keywords: Benzimidazole, piperazine, anticancer activity, A549 lung cancer, cytotoxicity, apoptosis

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(E-pub Ahead of Print)
DOI: 10.2174/1570180817999200513091613
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