Design and synthesis of benzimidazole-chalcone derivatives as potential anticancer agents

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Abstract

Numerous reports have shown that conjugated benzimidazole derivatives possess various kinds of biological activities, including anticancer properties. In this report, we designed and synthesized 24 new molecules comprising a benzimidazole ring, arene, and alkyl chain-bearing cyclic moieties. The results showed that the N-substituted benzimidazole derivatives bearing an alkyl chain and a nitrogen-containing 5- or 6-membered ring enhanced the cytotoxic effects on human breast adenocarcinoma (MCF-7) and human ovarian carcinoma (OVCAR-3) cell lines. Among the 24 synthesized compounds, (2E)-1-(1-(3-morpholinopropyl)-1H-benzimidazol-2 -yl)-3-phenyl-2-propen-1-one) (23a) reduced the proliferation of MCF-7 and OVCAR-3 cell lines demonstrating superior outcomes to those of cisplatin.

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Hsieh, C. Y., Ko, P. W., Chang, Y. J., Kapoor, M., Liang, Y. C., Chu, H. L., … Hsu, M. H. (2019). Design and synthesis of benzimidazole-chalcone derivatives as potential anticancer agents. Molecules, 24(18). https://doi.org/10.3390/molecules24183259

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