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Synthesis of novel aryl dithian valeryl podophyllotoxin ester derivatives as potential antitubulin agents

机译：新型芳基二硫杂戊戊基鬼臼毒素酯衍生物的合成作为潜在的抗微管蛋白剂

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Microtubules are among the most successful targets for anticancer therapy. In this study, we described the synthesis routes of the lipoyl podophyllotoxin ester derivatives and found that they can selectively inhibit the proliferation of cancer cells without damaging the non-cancer cells. Among them, L4 showed the best antiproliferation activity with IC50 = 2.68 mu M against A549 cells. This effect of L4 was similar to that of CA-4 ( IC50 = 2.78 mu M), a typical microtubule inhibitor, but better than podophyllotoxin ( IC50 = 6.57 mu M) itself. Furthermore, cell cycle analysis revealed that L4 can remarkably cause cell cycle arrest in the G2/M phase in a time- and dose-dependent manner. But the effect of L4 on apoptosis inducing was not apparent enough. Moreover, confocal microscopy and western blot analysis results indicated that L4 can perturb microtubule polymerization, thus causing tumor growth inhibition.
机译：微管是抗癌治疗最成功的靶标之一。在这项研究中，我们描述了脂酰鬼臼毒素酯衍生物的合成途径，并发现它们可以选择性地抑制癌细胞的增殖而不会损害非癌细胞。其中，L4对A549细胞表现出最佳的抗增殖活性，IC50 = 2.68μM。 L4的这种作用类似于典型的微管抑制剂CA-4的作用（IC50 = 2.78μM），但优于鬼臼毒素（IC50 = 6.57μM）本身。此外，细胞周期分析表明，L4可以以时间和剂量依赖性方式显着导致细胞周期阻滞在G2 / M期。但是L4对细胞凋亡诱导的作用还不够明显。此外，共聚焦显微镜和蛋白质印迹分析结果表明L4可以干扰微管聚合，从而引起肿瘤生长抑制。

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