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Design and Synthesis of Benzimidazole-Chalcone Derivatives as Potential Anticancer Agents.

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.

SUBMITTER: Hsieh CY

PROVIDER: S-EPMC6767017 | biostudies-literature | 2019 Sep

REPOSITORIES: biostudies-literature

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Design and Synthesis of Benzimidazole-Chalcone Derivatives as Potential Anticancer Agents.

Hsieh Cheng-Ying CY Ko Pi-Wen PW Chang Yu-Jui YJ Kapoor Mohit M Liang Yu-Chuan YC Lin Hui-Hsien HH Horng Jia-Cherng JC Hsu Ming-Hua MH

Molecules (Basel, Switzerland) 20190906 18

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 <i>N</i>-substituted benzimidazole derivatives bearing an alkyl chain and a nitrogen-containing 5- or 6-membered ring enhanced the cytotoxic effects on human breast adenocarcinoma ...[more]

PMID: 31500191

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