【摘 要】
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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 wer
【机 构】
:
Institute for Innovative Drug Design and Evaluation, School of Pharmacy, Henan University, Kaifeng 4
论文部分内容阅读
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 antiturnor activity and may become a promising candidate for future intensive study.
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