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

苯并咪唑-查尔酮衍生物作为潜在抗癌剂的设计和合成

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

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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