Key Laboratory of Pesticide & Chemical Biology, Ministry of Education, College of Chemistry, Central China Normal University, Wuhan 430079, PR China.
Eur J Med Chem. 2013 Aug;66:161-70. doi: 10.1016/j.ejmech.2013.05.037. Epub 2013 Jun 4.
As widely occurring natural products, flavonoids are an important source for drug discovery, due to their structural diversity and broad-spectrum biological activity. In this work, a library of novel, thioether-substituted flavonoids with diverse heterocyclic groups was synthesized via a microwave-assisted procedure with the advantages of good yields, short times, mild conditions and ready isolation of the products. Their antiproliferative activities were evaluated against six cancer cell lines, HCCLM-7, Hela, MDA-MB-435S, SW-480, Hep-2, and MCF-7 by the MTT-based assay. Compared with the positive control 5-fluorouracil, three compounds, 6a, 6b and 6j were successfully identified as the most promising candidates, due to their higher potency and broad-spectrum bioactivity with IC50 values in the range of 0.43 μM-6.7 μM.
作为广泛存在的天然产物，类黄酮因其结构多样性和广谱生物活性，成为药物发现的重要来源。在这项工作中，通过微波辅助方法合成了一系列新型的、含硫醚取代的、具有不同杂环基团的类黄酮化合物，该方法具有产率高、时间短、条件温和以及产物易于分离等优点。采用 MTT 比色法，以 5-氟尿嘧啶为阳性对照，评估了这些化合物对 HCCLM-7、Hela、MDA-MB-435S、SW-480、Hep-2 和 MCF-7 六种癌细胞系的增殖抑制活性。结果表明，与阳性对照物 5-氟尿嘧啶相比，化合物 6a、6b 和 6j 具有较高的活性和广谱的生物活性，IC50 值在 0.43 μM-6.7 μM 范围内，是最有前途的候选药物。
