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Design, synthesis and biological evaluation of benzimidazole–rhodanine conjugates as potent topoisomerase II inhibitors

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Abstract

In this study, a series of benzimidazole–rhodanine conjugates were designed, synthesized and investigated for their topoisomerase II (Topo II) inhibitory and cytotoxic activities. The results from Topo II-mediated pBR322 DNA relaxation and cleavage assays showed that the synthesized compounds might act as Topo II catalytic inhibitors. Certain compounds displayed potent Topo II inhibition at 10 μM. The cytotoxic activities of these compounds against HeLa, A549, Raji, PC-3, MDA-MB-201, and HL-60 cancer cell lines were evaluated. The results indicated that these compounds exhibited strong antiproliferative activity. A good relationship was observed between the Topo II inhibitory potency and the cytotoxicity of these compounds. The structure–activity relationship revealed that the electronic effects, the phenyl group, and the rhodanine moiety were particularly important for the Topo II inhibitory potency and cytotoxicity.

Graphical abstract: Design, synthesis and biological evaluation of benzimidazole–rhodanine conjugates as potent topoisomerase II inhibitors

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Publication details

The article was received on 03 Apr 2018, accepted on 01 Jun 2018 and first published on 02 Jun 2018


Article type: Research Article
DOI: 10.1039/C8MD00278A
Citation: Med. Chem. Commun., 2018, Advance Article
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    Design, synthesis and biological evaluation of benzimidazole–rhodanine conjugates as potent topoisomerase II inhibitors

    P. Li, W. Zhang, H. Jiang, Y. Li, C. Dong, H. Chen, K. Zhang and Z. Du, Med. Chem. Commun., 2018, Advance Article , DOI: 10.1039/C8MD00278A

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