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首页> 外文期刊>Journal of biological inorganic chemistry: JBIC: a publication of the Society of Biological Inorganic Chemistry >Metals in medicine: metal-related diseases-DNA binding and cytotoxic activity of Zn(II) and Cu(II) complexes with new bis(thiosemicarbazone) derivatives
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Metals in medicine: metal-related diseases-DNA binding and cytotoxic activity of Zn(II) and Cu(II) complexes with new bis(thiosemicarbazone) derivatives

机译：医药中的金属：与金属有关的疾病-Zn（II）和Cu（II）与新的双（thiosemicarbazone）衍生物的DNA结合和细胞毒活性

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Centro de Ciências e Tecnologias Nucleares-C~2TN, Instituto Superior Técnico, Universidade de Lisboa, Campus Tecnológico e Nuclear, Estrada Nacional 10, km 139.7, 2695-066 Bobadela, LRS-Portugal Bis(thiosemicarbazone) complexes of Zn(II) and Cu(II) have received considerable attention in the design of metallodrugs, either as anticancer therapeutics or diagnostic radiopharmaceuticals. Moreover, the availability of several medically relevant copper radioisotopes (e.g. ~(62)Cu, ~(64)Cu and ~(67)Cu) makes them potentially useful tools for cancer theranostics, profiting from a versatile chemical modification of the bis(thiosemicarbazone) framework and a stable coordination of radiocopper ions. The mechanism involved in the anticancer activity of Zn(II) and Cu(II) bis(thiosemicarbazonates) is not fully understood. However, it has been shown in a few studies that there is an accumulation of the complexes in the nucleus of tumor cells, indicating that DNA could be a potential target of their action. In this context, we have embarked in the synthesis of Zn(II) and Cu(II) complexes with new bis(thiosemicarbazone) chelators, symmetrically functionalized with protonable cyclic amines of the piperidine and morpholine type (Fig. 1). We have hypothesized that the presence of the cyclic amine groups could enhance the DNA affinity of the compounds and, together with the planarity of the metallic center, could promote some selectivity towards different types of DNA (e.g. G-quadruplex vs. duplex DNA). In this communication, we report the DNA binding and cytotoxic activity studies of these new M(II)-bis(thiosemicarbazone) complexes, performed with the aim of assessing their usefulness in the design of metal-based drugs for cancer theranostics.
机译：Centro deCiênciase Tecnologias Nucleares-C〜2TN，高等技术学院，里斯本大学，CampusTecnológicoe Nuclear，Estrada Nacional 10，km 139.7，2695-066 Bobadela，LRS-葡萄牙双（硫代半碳carb）络合物和Zn（II）和Cu（II）在金属药物的设计中已受到相当多的关注，无论是作为抗癌治疗剂还是诊断性放射性药物。此外，几种医学上相关的铜放射性同位素（例如〜（62）Cu，〜（64）Cu和〜（67）Cu）的可用性使它们成为癌症治疗学的潜在有用工具，得益于双（thiosemicarbazone）的多功能化学修饰）框架和放射性铜离子的稳定配合。 Zn（II）和Cu（II）双（硫代半氨基甲酸酯）的抗癌活性涉及的机制尚不完全清楚。然而，在一些研究中已经表明，肿瘤细胞的核中有复合物的积累，表明DNA可能是其作用的潜在靶标。在这种情况下，我们已着手合成具有新型双（硫代半碳zone）螯合剂的Zn（II）和Cu（II）配合物，并用哌啶和吗啉型的质子化环胺对称官能化（图1）。我们假设环胺基团的存在可以增强化合物的DNA亲和力，并与金属中心的平面性一起可以促进对不同类型DNA的某些选择性（例如G-四链体与双链体DNA）。在此通讯中，我们报告了这些新的M（II）-双（thiosemicarbazone）复合物的DNA结合和细胞毒性活性研究，目的是评估它们在设计用于癌症治疗的金属基药物中的有用性。

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