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Synthesis and Antitumor Activity of New Group 3 Metallocene Complexes

机译:新型3族金属茂配合物的合成及抗肿瘤活性

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摘要

The quest for alternative drugs with respect to the well-known cis-platin and its derivatives, which are still used in more than 50% of the treatment regimens for patients suffering from cancer, is highly needed. In this context, organometallic compounds, which are defined as metal complexes containing at least one direct covalent metal-carbon bond, have recently been found to be promising anticancer drug candidates. A series of new metallocene complexes with scandium, yttrium, and neodymium have been prepared and characterized. Some of these compounds show a very interesting anti-proliferative activity in triple negative breast cancer cell line (MDA.MB231) and the non-hormone sensitive prostate cancer cell line (DU145). Moreover, the interaction of some of them with biological membranes, evaluated using liposomes as bio-membrane mimetic model systems, seems to be relevant. The biological activity of these compounds, particularly those based on yttrium, already effective at low concentrations on both cancer cell lines, should be taken into account with regard to new therapeutic approaches in anticancer therapy.
机译:迫切需要寻找与众所周知的顺铂及其衍生物有关的替代药物,目前仍在50%以上的癌症患者治疗方案中使用该药物。在这种情况下,最近发现有机金属化合物定义为含有至少一个直接的共价金属-碳键的金属配合物,是有希望的抗癌药物候选物。已经制备和表征了一系列具有scan,钇和钕的新型茂金属配合物。这些化合物中的一些在三阴性乳腺癌细胞系(MDA.MB231)和非激素敏感性前列腺癌细胞系(DU145)中显示出非常有趣的抗增殖活性。此外,使用脂质体作为生物膜模拟模型系统评估了其中一些与生物膜的相互作用,似乎是相关的。这些化合物的生物活性,特别是基于钇的化合物,已经在两种癌细胞系中以低浓度有效,因此在抗癌治疗的新治疗方法中应予以考虑。

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