吖啶-多胺类缀合物的合成、抗肿瘤活性及与 DNA 键合作用

Synthesis,Antitumor Activity and DNA Binding of Acridine-polyamine Conjugates

设计合成了系列吖啶-多胺类衍生物（ACP1~ ACP6），并通过四甲基偶氮唑蓝（MTT）染色法研究了化合物对 K562（人白血病细胞）、 A549（人肺癌细胞）和 Hela（人宫颈癌细胞）细胞株的体外抗肿瘤活性。结果显示，化合物对肿瘤细胞具有一定的抑制作用，尤其是化合物 ACP2的抗肿瘤活性优于阳性对照顺铂。通过 UV-Vis 光谱、荧光光谱、圆二色谱和热变性实验研究了合成化合物与小牛胸腺 DNA（Ct-DNA）的键合作用。结果表明，三乙烯四胺修饰的化合物 ACP2具有较好的抗肿瘤活性，与 DNA 分子具有较强的结合能力。

A series of novel acridine-polyamine conjugates（ACP1-ACP6） was designed and synthesized. Their antitumor activities were evaluated against Leukemia cells（K562）, human lung cancer cells（A549） and human cervical carcinoma cells（Hela） in vitro using MTT assay. The results showed that compound ACP2 ex-hibited potent anticancer activities, which was better than the positive control drug（cis-platin）. Furthermore, their DNA binding properties were investigated by UV-Vis, fluorescence and circular dischroism（CD） spec-troscopies and thermal denaturation experiment, which showed that the acridine-polyamine conjugates as the DNA intercalator had strong binding interaction with Ct-DNA.