Synthesis and anti-tumor activities of quercetin and its derivatives / 中国药学杂志

ABSTRACT

OBJECTIVE: To design and synthesize series of quercetin derivatives by introducing allyl or prenyl groups and investigate their antitumor activities in vitro. METHODS: Compounds 2, 3, 4, 5, 6, 7 and 8 were synthesized with quercetin as starting material through the etherification reaction. The antitumor activities were evaluated by MTT assay against human lung cells (A549), human breast cancer cells (MDA-MB-231), and human hepatoma cells (HepG2). RESULTS: Two allyl-substituted and five prenyl-substituted quercetin derivatives were synthesized. Compounds 4, 5, 6, 7, and 8 were new compounds, and their structures were characterized by 1H-NMR and 13C-NMR. Compounds 6 and 7 exhibited observable anti-proliferative activity. Compound 6 inhibited the growth of A549, MDA-MB-231, and HepG2 cells with IC50 values of 15.23, 16.56, and 12.32 μmol·L-1, respectively. Compound 7 restrained the growth of A549 and MDA-MB-231 cells with IC50 values of 8.92 and 2.90 μmol·L-1, respectively. CONCLUSION: Compounds 6 and 7 synthesized by introducing prenyl groups into quercetin have significant anti-tumor activities, which are worth of further research.