Design, synthesis, and biological evaluation of novel nitric oxide releasing Dehydroandrographolide (cas 134418-28-3) derivatives

Add time:07/29/2019    Source:sciencedirect.com

A series of new hybrids of Dehydroandrographolide (cas 134418-28-3) (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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