Abstract Twelve novel aminoalkyl derivatives 3a-3f, 4a-4f and four novel amino acid derivatives 5a, 5b, 6a and 6b of polymethoxyflavones 1 and 2 were synthesized through regioselective demethylation, etherification, amination, EDCl-mediated amide condensation and alkaline hydrolysis, using tangeretin and nobiletin as starting materials. Their antiproliferative activities against four different human cancer cell lines (Aspc-1, SUN5, HepG-2 and HCT116) were evaluated by in vitro CCK-8 assay. The results show that the majority of the synthetic compounds exhibited moderate to good antiproliferative activity. In particular, the antiproliferative activity of compound 5b against HepG-2 cells (IC50 0.057 μM) was equal to the positive control drug Staurosporine (IC50 0.0575 μM).

中文翻译：

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多甲氧基黄酮氨烷基及氨基酸衍生物的合成及抗增殖活性

摘要 通过区域选择性去甲基化、醚化、胺化、EDCl 介导的酰胺缩合和碱水解，合成了聚甲氧基黄酮 1 和 2 的 12 种新型氨基烷基衍生物 3a-3f、4a-4f 和 4 种新型氨基酸衍生物 5a、5b、6a 和 6b。以橘皮苷和川陈皮苷为起始原料。通过体外 CCK-8 测定评估它们对四种不同人类癌细胞系（Aspc-1、SUN5、HepG-2 和 HCT116）的抗增殖活性。结果表明，大多数合成化合物表现出中等至良好的抗增殖活性。特别地，化合物5b对HepG-2细胞的抗增殖活性(IC50 0.057 μM)等于阳性对照药物星形孢菌素(IC50 0.0575 μM)。