首页> 外文期刊>Polyhedron: The International Journal for Inorganic and Organometallic Chemistry >A new pyrazolone based ternary Cu(II) complex: Synthesis, characterization, crystal structure, DNA binding, protein binding and anti-cancer activity towards A549 human lung carcinoma cells with a minimum cytotoxicity to non-cancerous cells
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A new pyrazolone based ternary Cu(II) complex: Synthesis, characterization, crystal structure, DNA binding, protein binding and anti-cancer activity towards A549 human lung carcinoma cells with a minimum cytotoxicity to non-cancerous cells

机译:一种新型的吡唑啉酮三元铜(II)配合物:对A549人肺癌细胞的合成,表征,晶体结构,DNA结合,蛋白质结合和抗癌活性,对非癌细胞的细胞毒性最小

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摘要

With the aim of exploring the anticancer properties of coordination compounds, we report for the first time the synthesis of the new ternary complex [Cu(TMCPMP-TS)(Phen)] (TMCPMP-TS; (Z)-2-((1-(3-chlorophenyl)-3-methyl-5-oxo-4, 5-dihydro-1H-pyrazol-4-yl)(p-tolyl)methylene) hydrazinecarbothioamide and Phen; 1,10-phenanthroline). The complex was characterized by various techniques, including X-ray crystallography which showed that the geometry of the metal centre was between square pyramidal and trigonal bipyramidal. The interaction with calf-thymus DNA showed binding through intercalation. The protein binding ability with bovine serum albumin revealed a stronger binding of complex as compared to the free ligands. The anticancer activity of the complex was investigated by exposing it to the A549 (human lung cancer) cell line, which showed mitochondrial damage via an oxidative mechanism. After 24 h treatment, the complex arrested S and G2/M phases in the cell cycle progression and induced cell death. The results envisaged herein indicate that Cu(TMCPMP-TS)(Phen) holds ample merit to develop it as a therapeutic agent against cancer.
机译:为了探索配位化合物的抗癌特性,我们首次报道了新的三元复合物[Cu(TMCPMP-TS)(Phen)](TMCPMP-TS;(Z)-2-((1 -(3-氯苯基)-3-甲基-5-氧代-4、5-二氢-1H-吡唑-4-基)(对甲苯基亚甲基)肼基甲硫基酰胺和苯; 1,10-菲咯啉)。该配合物通过各种技术进行表征,包括X射线晶体学分析,该技术表明金属中心的几何形状介于方形金字塔形和三角形双锥体之间。与小牛-胸腺DNA的相互作用显示出通过结合的结合。与游离配体相比,与牛血清白蛋白的蛋白结合能力显示出更强的复合物结合。通过将复合物暴露于A549(人肺癌)细胞系中来研究其抗癌活性,该细胞系通过氧化机制显示线粒体损伤。处理24小时后,该复合物在细胞周期进程中停止了S和G2 / M期,并诱导了细胞死亡。本文设想的结果表明,Cu(TMCPMP-TS)(Phen)具有充分的优点,可将其开发为抗癌治疗剂。

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