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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Synthesis, characterization, DFT calculation and biological activity of square-planar Ni(II) complexes with tridentate PNO ligands and monodentate pseudohalides. Part II
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Synthesis, characterization, DFT calculation and biological activity of square-planar Ni(II) complexes with tridentate PNO ligands and monodentate pseudohalides. Part II

机译:具有三齿PNO配体和单齿假卤化物的方平面Ni(II)配合物的合成,表征,DFT计算和生物活性。第二部分

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Three square-planar complexes of Ni(II) with condensation derivative of 2-(diphenylphosphino)benzaldehyde and 4-phenylsemicarbazide and monodentate pseudohalides have been synthesized and characterized on the basis of the results of X-ray. NMR and IR spectroscopy and elemental analysis. Investigated complexes exhibited moderate antibacterial and cytotoxic activity. The most pronounced cytotoxic activity (in the range of cisplatin) to HeLa cell line was observed for ligand and all the complexes. Azido complex and ligand induced concentration dependent cell cycle arrest in the S phase, as well as decrease of percentage of cells in G1 phase, without significant increase of apoptotic fraction of cells. The interaction of the azido complex and ligand with CT-DNA results in changes in UV-Vis spectra typical for non-covalent bonding. The observed intrinsic binding constant of azido complex CT-DNA and ligand-CT-DNA were 3.22 x 10(5) M-1 and 2.79 x 10(5) M-1. The results of DNA cleavage experiments showed that azido complex nicked supercoiled plasmid DNA. (C) 2014 Elsevier Masson SAS. All rights reserved.
机译:根据X射线的结果,合成了Ni(II)与2-(二苯基膦基)苯甲醛和4-苯基氨基脲的缩合衍生物和单齿假卤化物的三个方形平面络合物。 NMR和IR光谱学和元素分析。研究的复合物表现出中等的抗菌和细胞毒性活性。对于配体和所有复合物,观察到对HeLa细胞系最明显的细胞毒活性(在顺铂范围内)。叠氮基复合物和配体诱导的浓度依赖性细胞周期阻滞在S期,以及G1期细胞百分比的降低,而细胞凋亡分数却没有明显增加。叠氮基络合物和配体与CT-DNA的相互作用导致典型的非共价键合UV-Vis光谱变化。所观察到的叠氮基复合物CT-DNA和配体-CT-DNA的固有结合常数为3.22×10(5)M-1和2.79×10(5)M-1。 DNA切割实验的结果表明叠氮基复合物切口超螺旋质粒DNA。 (C)2014 Elsevier Masson SAS。版权所有。

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