Abstract
AbstractA series of combretastatin A‐4 based chalcones (14a‐l) were designed, synthesized and these compounds examined for inhibitory effects on the proliferation of human lung (A549), breast (MCF‐7), melanoma (A375), and colon (HT‐29) carcinoma cells. Compounds 14b, 14c, 14e, 14h, and 14i (tri/dimethoxy, methyl, and mono/dinitro derivatives) have exhibited the most potent antiproliferative activity with IC50 < 2 μM and the hexa methoxy derivative 14b, the most promising one, which displayed the potent inhibitory activities in MCF‐7 (IC50: 10 nM), A375 (IC50: 12 nM), and A549 (IC50: 65 nM) cell lines, and is 18 times more potent than the CA‐4. Compound 14b represents a new scaffold and the results provide insights into further development of anticancer agents.
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