Design, synthesis and biological evaluation of novel furoxan-based coumarin derivatives as antitumor agents

AbstractIn order to find new anticancer drugs, a series of novel furoxan-based coumarin derivatives (10a–k) were synthesized and evaluated for their antiproliferative activities in vitro. All compounds displayed more potent inhibition on human cervical cancer HeLa cell proliferation than coumarin-3-carboxylic acid, and compounds10b, 10c, 10f, 10h, and10i with IC50 values ranging from 0.88 to 5.95  μM were even stronger than doxorubicin (IC50 = 10.21 μM). The further study showed that compound10i exerted the highest antiproliferative activity (IC50 = 0.60 μM) against human breast cancer MCF-7 cells, and compound10f had broader spectrum antiproliferative activity against five cancer cells with IC50 values in the low micromolar range of 1.86 –9.85 μM. More interestingly, compound10f had little effect on normal intestinal epithelial CCD841 cells. Our findings suggest that these novel furoxan-based coumarin derivatives may provide a new framework for the discovery of novel antitumor agents for the intervention of human carcinoma cells.
Source: Medicinal Chemistry Research - Category: Chemistry Source Type: research

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