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

2019; Multidisciplinary Digital Publishing Institute; Volume: 24; Issue: 18 Linguagem: Inglês

10.3390/molecules24183259

1433-1373

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,

Bioactive Compounds and Antitumor Agents

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.