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Selenoesters and selenoanhydrides as novel multidrug resistance reversing agents: A confirmation study in a colon cancer MDR cell line

机译:硒酸酯和硒代酸酐作为新型多药耐药逆转剂:在结肠癌MDR细胞系中的一项确认研究

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摘要

Taking into account that multidrug resistance (MDR) is the main cause for chemotherapeutic failure in cancer treatment and as a continuation of our efforts to overcome this problem we report the evaluation of one cyclic selenoanhydride (1) and ten selenoesters (2-11) in MDR human colon adenocarcinoma Colo 320 cell line. The most potent derivatives (1, 9-11) inhibited the ABCB1 efflux pump much stronger than the reference compound verapamil. Particularly, the best one (9) was 4-fold more potent than verapamil at a 10-fold lower concentration. Furthermore, the evaluated derivatives exerted a potent and selective cytotoxic activity. In addition, they were strong apoptosis inducers as the four derivatives triggered apoptotic events in a 64-72% of the examined MDR Colo 320 human adenocarcinoma cells.
机译:考虑到多药耐药性(MDR)是癌症治疗中化疗失败的主要原因,因此,作为我们克服这一问题的努力的继续,我们报告了对一种环硒代酸酐(1)和十种硒酸酯(2-11)的评估。 MDR人结肠腺癌Colo 320细胞系。最有效的衍生物(1、9-11)对ABCB1外排泵的抑制作用比参考化合物维拉帕米强得多。特别是,最好的一种(9)在低10倍的浓度下比维拉帕米强4倍。此外,所评价的衍生物发挥了有效的和选择性的细胞毒性活性。此外,它们是强凋亡诱导剂,因为这四种衍生物在64-72%的MDR Colo 320人腺癌细胞中触发了凋亡事件。

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