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Some ferrocenyl chalcones as useful candidates for cancer treatment

机译:一些二茂铁基查耳酮可作为治疗癌症的有用候选药物

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Although knowledge of cancer management is extensive, mortality is not currently declining in this area. It is therefore important to implement a long-term strategy that would aim to prevent these serious diseases. Ferrocene-related organometallic compounds are promising candidates for design of new drugs since they can exhibit much greater biological activity than their phenyl analogs. In our work, we focused on investigating the cytotoxic and antiproliferative effects of five ferrocenyl derivatives toward selected tumor cell lines. We found that some of these substances significantly reduced Jurkat cell survival and, to a lesser extent, that of the HeLa, MCF7, A549, and MDA cells. Long-term treatment of HeLa cell cultures with these agents resulted in a significant blockade of formation of tumor cell colonies. We found that one of the mechanisms of action of the compounds is likely to display an effect on the redox state of the mitochondria at a final concentration of 10(-4) and 10(-5) mol l(-1). Of the compounds tested, the indanonyl ferrocene derivative (C) was the most effective, especially via glutathione depletion. Based on the obtained results, it can be concluded that synthetic substances containing iron have potential antitumor activity.
机译:尽管癌症管理的知识广博,但该领域的死亡率目前并未下降。因此,重要的是执行旨在预防这些严重疾病的长期策略。二茂铁相关的有机金属化合物是新药设计的有希望的候选者,因为它们比其苯基类似物具有更大的生物活性。在我们的工作中,我们专注于研究五种二茂铁基衍生物对选定的肿瘤细胞系的细胞毒性和抗增殖作用。我们发现其中一些物质显着降低了Jurkat细胞的存活率,并在较小程度上降低了HeLa,MCF7,A549和MDA细胞的存活率。用这些试剂对HeLa细胞培养物进行长期处理会显着阻止肿瘤细胞集落的形成。我们发现,化合物的作用机理之一很可能在最终浓度为10(-4)和10(-5)mol l(-1)时对线粒体的氧化还原状态产生影响。在测试的化合物中,茚满壬基二茂铁衍生物(C)最有效,尤其是通过谷胱甘肽耗竭。根据获得的结果,可以得出结论,含铁的合成物质具有潜在的抗肿瘤活性。

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