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Synthesis, crystal structure, nuclease and in vitro antitumor activities of a new mononuclear copper(II) complex containing a tripodal N3O ligand

机译:含有三脚架N3O配体的新型单核铜(II)配合物的合成,晶体结构,核酸酶和体外抗肿瘤活性

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We present here the synthesis, crystal structure, electrochemical behavior, spectroscopic properties (FT-IR, LJ-V-Vis and EPR), nuclease and in vitro antitumor activities against human myeloid leukemia cell line of the mononuclear copper complex [Cu(HPClNOL)(Cl)]Cl (.) MeOH (1). The reaction of the tetradentate ligand HPClNOL [1-(bis-pyridin-2-ylmethyl-amino)-3-chloropropan-2-ol] and 1 equiv. of [Cu(OH2)(6)](Cl)(2), in methanol, resulted in 1, which crystallizes as blue monoclinic crystals. The complex is pentacoordinated with a distorted square-pyramidal geometry. The activity of complex 1 toward plasmid DNA and THP-1 carcinogenic cells was investigated. Complex I promotes the cleavage of supercoiled DNA (pBlueScript KS+ DNA) to nicked circular and linear DNA forms. In addition to the three typical KS+ DNA forms, the cleavage resulted in a fourth band, which was visualized above of the nicked circular form. The results reveal that the cleavage mechanism is radical-independent. Furthermore, complex I is able to promote cell death of THP-1 cells by apoptosis, as confirmed by fluorescent microscopy, cell morphology and DNA degradation. (c) 2006 Elsevier B.V. All rights reserved.
机译:我们在这里介绍合成,晶体结构,电化学行为,光谱性质(FT-IR,LJ-V-Vis和EPR),核酸酶和体外抗肿瘤活性对人类髓样白血病细胞系的单核铜络合物[Cu(HPClNOL) (Cl)] Cl(。)MeOH(1)。四齿配体HPClNOL [1-(双吡啶-2-基甲基-氨基)-3-氯丙烷-2-醇]与1当量的反应。在甲醇中溶解[Cu(OH2)(6)](Cl)(2),得到1,其结晶为蓝色单斜晶体。该复合体以扭曲的方金字塔形几何体五角坐标。研究了复合物1对质粒DNA和THP-1致癌细胞的活性。复合物I促进超螺旋DNA(pBlueScript KS + DNA)的裂解为有缺口的环状和线性DNA形式。除了三种典型的KS + DNA形式外,切割还产生了第四条带,该条带在带锯齿的圆形上方可见。结果表明,裂解机理是自由基无关的。此外,如荧光显微镜,细胞形态和DNA降解所证实,复合物I能够通过凋亡促进THP-1细胞的细胞死亡。 (c)2006 Elsevier B.V.保留所有权利。

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