A series of eleven 9-acridinyl amino acid derivatives were synthesized using a two-step procedure. Cytotoxicity was tested on the K562 and A549 cancer cell lines and normal diploid cell line MRC5 using the MTT assay. Compounds 6, 7, 8 and 9 were the most active, with IC₅₀ values comparable to or lower than that of chemotherapeutic agent amsacrine. 8 and 9 were especially effective in the A549 cell line (IC₅₀ ≈ 6 μM), which is of special interest since amsacrine is not sufficiently active in lung cancer patients. Cell cycle analysis revealed that 7 and 9 caused G2/M block, amsacrine caused arrest in the S phase, while 6 and 8 induced apoptotic cell death independently of the cell cycle regulation. In comparison to amsacrine, 6, 7, 8, and 9 showed similar inhibitory potential towards topoisomerase II, whereas only 7 showed DNA intercalation properties. In contrast to amsacrine, 6, 7, 8 and 9 showed a lack of toxicity towards unstimulated normal human leucocytes.

中文翻译：

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新的9-ac啶基氨基酸衍生物的合成及其抗癌活性

使用两步法合成了一系列11种9--啶基氨基酸衍生物。使用MTT测定法在K562和A549癌细胞系和正常二倍体细胞系MRC5上测试了细胞毒性。化合物6，7，8和9是最活跃的，具有IC _50个值相当或比化学治疗剂安吖啶的降低。8和9分别为在A549细胞系（IC是特别有效的₅₀ ≈6μM），这是特别令人感兴趣的，因为安吖啶是不是在肺癌患者具有足够的活性。细胞周期分析显示7和9导致G2 / M阻滞，氨苯磺酸导致S期阻滞，而6和8则独立于细胞周期调控而诱导凋亡性细胞死亡。相比于安吖啶，6，7，8，和9显示出朝向拓扑异构酶II类似的抑制潜力，而只有7表明DNA嵌入性质。与此相反，以安吖啶，6，7，8和9显示出缺乏对未刺激的正常人白细胞毒性。