Synthesis and Antiproliferative Activity of Natural and Non-Natural Polymethoxychalcones and Polymethoxyflavones

摘要

Two series of polymethoxychalcones and polymethoxyflavones, including the natural products 2-hydroxy-3,4,5,4,6-pentamethoxychalcone (8c), 5,6,7,8,3,4,5-heptamethoxyflavone (6), 5,7,3,4,5-pentamethoxyflavone (9c), 3-hydroxy-5,6,7,8,3,4,5-heptamethoxyflavone (7), and 3-hydroxy-5,7,3,4,5-pentamethoxyflavone (10), were synthesized. The antiproliferative activity in vitro was evaluated against a panel of three human cancer cell lines (HeLa, HCC1954, and SK-OV-3) by the cell counting kit-8 (CCK-8) assay. The results showed that most of the synthetic compounds exhibited moderate to potent antiproliferative activities. Some compounds displayed equal or higher potential than the positive control drug cisplatin. In particular, compounds 4c, 4e, 8a, and 9a possess IC50 values equal to or below 10 M and are worthy of further investigation.