Abstract
A series of four 3-acyl-5-hydroxybenzofuran derivatives (4a-4d) were synthesized by one-pot method under microwave irradiation from aldehydes, dimethylformamide dimethyl acetal (DMFA) and benzoquinone in high yields. These compounds were characterized by IR, NMR and ESI-MS, which were also tested for in vitro anti-proliferative activity against human breast cancer ER(+)-MCF-7 and ER(-)-MDA-MB-231 cell lines. The bioactive compound 4d exhibited the best anti-breast cancer activity against MCF-7 cells with the IC50 values of 43.08 μM. The compound might be used as a potential anti-tumor agent for the further structure modifications and development.
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