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基于银的三联吡啶配合物作为抗肿瘤剂。

Silver-Based Terpyridine Complexes as Antitumor Agents.

机构信息

Departamento de Química, Universidad de La Rioja, Centro de investigación de Síntesis Química (CISQ), Complejo Científico-Tecnológico, 26004-, Logroño, Spain.

Departamento de Bioquímica y Biología Celular, Universidad de Zaragoza-CSIC, 50009, Zaragoza, Spain.

出版信息

Chemistry. 2023 Jul 3;29(37):e202300116. doi: 10.1002/chem.202300116. Epub 2023 May 9.

Abstract

Silver complexes bearing substituted terpyridine or tetra-2-pyridinylpyrazine ligands have been prepared and structurally characterised. The study of the anticancer properties of silver complexes with this type of ligands is scarce, despite the possibilities of combining the properties of the metal and the ability of the ligands for DNA binding. Here, the antiproliferative activity, stability, CT-DNA binding, and mechanism of cell death of these types of derivatives are studied. High cytotoxicity against different tumour cells was observed, and, more important, a great selectivity index has been detected between tumour cells and healthy lymphocytes T for some of these compounds. The CT-DNA interaction study has shown that these derivatives are able to interact with CT-DNA by moderate intercalation. Furthermore, cell death studies indicate that these derivatives promote the apoptosis by a mitochondrial pathway.

摘要

合成了含有取代的三吡啶或四-2-吡啶基吡嗪配体的银配合物,并对其结构进行了表征。尽管金属的性质和配体与 DNA 结合的能力可以结合,但具有这种类型配体的银配合物的抗癌性质的研究却很少。在这里,研究了这些衍生物的抗增殖活性、稳定性、与 CT-DNA 的结合以及细胞死亡的机制。观察到对不同肿瘤细胞的高细胞毒性,更重要的是,对于这些化合物中的一些,在肿瘤细胞和健康 T 淋巴细胞之间检测到了非常高的选择性指数。CT-DNA 相互作用研究表明,这些衍生物能够通过适度的嵌入与 CT-DNA 相互作用。此外,细胞死亡研究表明,这些衍生物通过线粒体途径促进细胞凋亡。

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