Microwave-Assisted Synthesis and Anti-Breast Cancer Activity of 3-Acyl-5-hydroxybenzofurans

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.