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

Author:
Vongdeth, Kingsadingthongkham, Han, Peipei, Li, Wei, Wang, Qiu-An
Source:
Chemistry of natural compounds 2019 v.55 no.1 pp. 11-17
ISSN:
0009-3130
Subject:
chemistry, cisplatin, human cell lines, humans, inhibitory concentration 50, neoplasm cells, polymethoxyflavones
Abstract:
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 μM and are worthy of further investigation.
Agid:
6332318