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首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >Selenoesters and selenoanhydrides as novel multidrug resistance reversing agents: A confirmation study in a colon cancer MDR cell line
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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:Selenoesters和硒酐作为新型多药耐性逆转剂:结肠癌MDR细胞系的确认研究

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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. (C) 2017 Elsevier Ltd. All rights reserved.
机译:考虑到多药耐药性(MDR)是癌症治疗中化学治疗失败的主要原因,作为我们努力克服这一问题的延续,我们报告了对一个环状硒酐(1)和10个Selenoesters(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)抑制了ABCB1 Efflux泵比参考复合维拉帕米更强大。 特别是,最佳(9)的浓度高出4倍,浓度为10倍。 此外,评估的衍生物施加有效和选择性的细胞毒性活性。 此外,它们是强凋亡的诱导剂,因为四种衍生物在64-72%的检测的MDR Colo 320人腺癌细胞中引发凋亡事件。 (c)2017 Elsevier Ltd.保留所有权利。

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