Design, synthesis, and biological evaluation of novel nitric oxide releasing dehydroandrographolide derivatives

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Abstract

A series of new hybrids of dehydroandrographolide (TAD), a biologically active natural product, bearing nitric oxide (NO)-releasing moieties were synthesized and designated as NO-donor dehydroandrographolide. The biological activities of target compounds were studied in human erythroleukemia K562 cells and breast cancer MCF-7 cells. Biological evaluation indicated that the most active compound I-5 produced high levels of NO and inhibited the proliferation of K562 (IC50 1.55 μmol·L−1) and MCF-7 (IC50 2.91 μmol·L−1) cells, which were more potent than the lead compound TAD and attenuated by an NO scavenger. In conclusion, I-5 is a novel hybrid with potent antitumor activity and may become a promising candidate for future intensive study.

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    Available online 20 Oct., 2018

    [Research funding] This work was supported by the National Natural Science Foundation of China (Nos. 81673299 and U1704185) and the Science and Technology Opening and Co-production Project of Henan Province of China (182106000060).

    These authors have no conflict of interest to declare.

    Δ

    These three authors contributed equally to this work.

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