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Synthesis, crystal structures and biological evaluation of three ternary copper(II) complexes with fluorinated anthranilic acid derivatives

机译:含氟邻氨基苯甲酸衍生物的三种三元铜(Ⅱ)配合物的合成,晶体结构和生物学评价

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摘要

Three ternary copper(II) complexes [Cu(L-1)(phen)] (1), [Cu(L-2)(phen)] (2), and [Cu(L-3)(phen)]center dot 2H(2)O (3) (L-1 = 4-fluoro-2-(picolinamido)benzoic acid, L-2 = 4,5-difluoro-2-(picolinamido)benzoic acid, L-3 = 4,5-difluoro-2-((2-hydroxybenzylidene)amino)benzoic acid, phen = 1,10-phenanthroline) have been synthesized and characterized by physicochemical and spectroscopic methods. In addition, X-ray crystallography showed that the Cu atoms in each of the complexes are five-coordinate, adopting distorted square pyramidal or trigonal bipyramidal geometries. The interactions of the complexes with calf-thymus DNA were investigated by UV absorption, fluorescence spectroscopy and viscosity measurements. In addition, the complexes were screened for in vitro cytotoxicity against A549 (human pulmonary carcinoma cells), Jurkat (human T lymphocyte cell line) and HepG-2 (human liver hepatocellular carcinoma cells); these experiments showed that complex 3 exhibited the most effective cytotoxicities (IC50 = 1.224-7.099 A mu M). Antibacterial studies revealed that complex 3 also exhibited highest activity, consistent with the DNA binding affinities.
机译:三个三元铜(II)配合物[Cu(L-1)(phen)](1),[Cu(L-2)(phen)](2)和[Cu(L-3)(phen)]中心点2H(2)O(3)(L-1 = 4-氟-2-(吡啶并氨基)苯甲酸,L-2 = 4,5-二氟-2-(吡啶并氨基)苯甲酸,L-3 = 4,合成了5-二氟-2-((2-羟基苄叉基)氨基)苯甲酸,phen = 1,10-菲咯啉,并通过物理化学和光谱法对其进行了表征。另外,X射线晶体学表明,每个配合物中的Cu原子是五坐标的,采用扭曲的方形金字塔或三角形双锥体的几何形状。通过紫外线吸收,荧光光谱和粘度测量研究了配合物与小牛胸腺DNA的相互作用。另外,筛选复合物对A549(人肺癌细胞),Jurkat(人T淋巴细胞细胞系)和HepG-2(人肝肝细胞癌细胞)的体外细胞毒性。这些实验表明,复合物3表现出最有效的细胞毒性(IC50 = 1.224-7.099 AμM)。抗菌研究表明,复合物3的活性最高,与DNA结合亲和力一致。

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