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首页> 外文期刊>Dalton transactions: An international journal of inorganic chemistry >Copper(i) and nickel(ii) complexes with 1:1 vs. 1:2 coordination of ferrocenyl hydrazone ligands: Do the geometry and composition of complexes affect DNA binding/cleavage, protein binding, antioxidant and cytotoxic activities?
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Copper(i) and nickel(ii) complexes with 1:1 vs. 1:2 coordination of ferrocenyl hydrazone ligands: Do the geometry and composition of complexes affect DNA binding/cleavage, protein binding, antioxidant and cytotoxic activities?

机译：具有二茂铁enyl配体的1：1和1：2配位的铜（i）和镍（ii）配合物：配合物的几何形状和组成是否影响DNA结合/裂解，蛋白质结合，抗氧化剂和细胞毒性活性？

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摘要

A new series of geometrically different complexes containing ferrocenyl hydrazone ligands were synthesised by reacting suitable precursor complex [MCl _2(PPh _3) _2] with the ligands HL ~1 or HL ~2 (where M = Cu(ii) or Ni(ii); HL ~1 = [Cp _2Fe(CHN-NH -CO- C _6H _5)] (1) and HL ~2 = [Cp _2Fe(CHN-NH-CO-C _5H _4N)]) (2). The new complexes of the composition [Cu(L ~1)(PPh _3) _2], (3) [Cu(L ~2)(PPh _3) _2] (4), [Ni(L ~1) _2] (5) and [Ni(L ~2) 2] (6) were characterised by various spectral studies. Among them, complexes 3 and 5 characterised by single crystal X-ray diffraction showed a distorted tetrahedral structure for the former with 1:1 metal-ligand stoichiometry, but a distorted square planar geometry with 1:2 metal-ligand stoichiometry in the case of the latter. Systematic biological investigations like DNA binding, DNA cleavage, protein binding, free radical scavenging and cytotoxicity activities were carried out using all the synthesised compounds and the results obtained were explained on the basis of structure-activity relationships. The binding constant (K _b) values of the synthesised compounds are found to be in the order of magnitude 10 ~3-10 ~5 M ~(-1) and also they exhibit significant cleavage of supercoiled (SC) pUC19 DNA in the presence of H _2O _2 as co-oxidant. The conformational changes of bovine serum albumin (BSA) upon binding with the above complexes were also studied. In addition, concentration dependent free radical scavenging potential of all the synthesised compounds (1-6) was also carried out under in vitro conditions. Assays on the cytotoxicity of the above complexes against HeLa and A431 tumor cells and NIH 3T3 normal cells were also carried out.
机译：通过使合适的前体络合物[MCl _2（PPh _3）_2]与配体HL〜1或HL〜2（其中M = Cu（ii）或Ni（ii））反应，合成了一系列新的含二茂铁enyl配体的几何不同配合物; HL〜1 = [Cp _2Fe（CHN-NH -CO-C _6H _5）]（1）和HL〜2 = [Cp _2Fe（CHN-NH-CO-C _5H _4N）]）（2）。组成为[Cu（L〜1）（PPh _3）_2]，（3）[Cu（L〜2）（PPh _3）_2]（4），[Ni（L〜1）_2]（ 5）和[Ni（L〜2）2]（6）通过各种光谱研究表征。其中，以单晶X射线衍射为特征的配合物3和5在金属配体化学计量比为1：1的情况下显示出扭曲的四面体结构，而在金属配体化学计量比为1：2的情况下显示出扭曲的正方形平面几何形状。后者。使用所有合成的化合物进行了系统的生物学研究，例如DNA结合，DNA裂解，蛋白质结合，自由基清除和细胞毒性活性，并根据结构-活性关系解释了获得的结果。发现合成化合物的结合常数（K _b）值在10〜3-10〜5 M〜（-1）的数量级，并且在存在下它们也显示出超螺旋（SC）pUC19 DNA的显着裂解。 H _2O _2作为助氧化剂。还研究了与上述复合物结合后牛血清白蛋白（BSA）的构象变化。此外，还在体外条件下进行了所有合成化合物（1-6）的浓度依赖性自由基清除潜能。还测定了上述复合物对HeLa和A431肿瘤细胞和NIH 3T3正常细胞的细胞毒性。

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