| In this study, a series of structurally novel 3-aryl-7,8-furanocoumarin derivatives were synthesized, and their in vitro antitumor activities were evaluated. Using 2,4-dihydroxybenzaldehyde and substituted phenylacetic acid as starting materials, the target compounds 3a–3i were prepared through nucleophilic substitution, Claisen rearrangement, Perkin condensation, and subsequent cyclization reactions. The structures of the products were confirmed by NMR, MS, and X-ray single-crystal diffraction. Activity screening results showed that compounds 3d, 3e, and 3g exhibited strong inhibitory effects against HeLa cells, with IC?? values of (22.68±1.68), (18.24±0.26), and (19.26±0.76) μM, respectively. Among these, compound 3e exhibited inhibitory activity against HepG2 and MCF-7 cells (IC?? values of 4.41±0.18 μM and 25.85±1.59 μM, respectively) comparable to that of cisplatin; however, it exhibited some toxicity toward normal LO2 liver cells. This study lays the experimental foundation for subsequent structural modification and mechanism studies of this class of furanocoumarin derivatives as novel anti-tumor lead compounds. |
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