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

Cheng Ying Hsieh, Pi Wen Ko, Yu Jui Chang, Mohit Kapoor, Yu Chuan Liang, Hsueh Liang Chu, Hui Hsien Lin, Jia Cherng Horng, Ming Hua Hsu

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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.

Original languageEnglish
Article number3259
JournalMolecules
Volume24
Issue number18
DOIs
Publication statusPublished - 2019 Sep 6

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All Science Journal Classification (ASJC) codes

  • Analytical Chemistry
  • Chemistry (miscellaneous)
  • Molecular Medicine
  • Pharmaceutical Science
  • Drug Discovery
  • Physical and Theoretical Chemistry
  • Organic Chemistry

Cite this

Hsieh, C. Y., Ko, P. W., Chang, Y. J., Kapoor, M., Liang, Y. C., Chu, H. L., Lin, H. H., Horng, J. C., & Hsu, M. H. (2019). Design and synthesis of benzimidazole-chalcone derivatives as potential anticancer agents. Molecules, 24(18), [3259]. https://doi.org/10.3390/molecules24183259