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Issue 6, 2017
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Design, synthesis and pharmacological evaluation of new 2-oxo-quinoline derivatives containing α-aminophosphonates as potential antitumor agents

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Abstract

A series of novel 2-oxo-quinoline derivatives containing α-aminophosphonates were designed and synthesized as antitumor agents. MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay results demonstrated that some compounds exhibited moderate to high inhibitory activity against HepG2, SK-OV-3 and NCI-H460 tumor cell lines, and most compounds showed much lower cytotoxicity against HL-7702 normal cells than 5-FU and cisplatin. The action mechanism of representative compound 5b was investigated by fluorescence staining assay, flow cytometric analysis and western blot (WB) assay, which indicated that this compound induced apoptosis and G2/M phase arrest accompanied by an increase in the production of intracellular Ca2+ and reactive oxygen species (ROS) and affecting associated enzymes and genes.

Graphical abstract: Design, synthesis and pharmacological evaluation of new 2-oxo-quinoline derivatives containing α-aminophosphonates as potential antitumor agents

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Publication details

The article was received on 25 Feb 2017, accepted on 29 Mar 2017 and first published on 31 Mar 2017


Article type: Research Article
DOI: 10.1039/C7MD00098G
Citation: Med. Chem. Commun., 2017,8, 1158-1172
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    Design, synthesis and pharmacological evaluation of new 2-oxo-quinoline derivatives containing α-aminophosphonates as potential antitumor agents

    Y. Yu, W. Kuang, R. Huang, Y. Fang, Y. Zhang, Z. Chen and X. Ma, Med. Chem. Commun., 2017, 8, 1158
    DOI: 10.1039/C7MD00098G

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