首页> 外文期刊>Journal of Inorganic Biochemistry: An Interdisciplinary Journal >Complexes of N-hydroxyethyl-N-benzimidazolylmethylethylenediaminediacetic acid with group 12 metals and vanadium-Synthesis, structure and bioactivity of the vanadium complex
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Complexes of N-hydroxyethyl-N-benzimidazolylmethylethylenediaminediacetic acid with group 12 metals and vanadium-Synthesis, structure and bioactivity of the vanadium complex

机译:N-羟乙基-N-苯并咪唑基甲基乙二胺二乙酸与十二族金属和钒的配合物-钒配合物的合成,结构和生物活性

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摘要

Four new complexes of group 12 metals [Zn(II), Cd(II) and Hg(II)], along with vanadyl bound to the ligand N-hydroxyethyl-N-benzimidazolylmethylethylenediaminediacetic acid, have been synthesized and characterized. The structure of the complexes with Zn(II), Hg(II) and V(IV) was determined by X-ray structural analysis. In all observed cases, the symmetry of these complexes was found to be distorted octahedral. The inhibition of protein tyrosine phosphatase 1B by the vanadium(IV) complex was demonstrated. The cytotoxicity of the vanadium(IV) complex was tested in vitro against three cancer cell lines, with a comparison of the activity of the free ligand and of vanadyl acetylacetonate and sodium orthovanadate. The IC50 values of the complex were in the range of 9 to 21 mu M. Remarkably, cytotoxic potency in the multidrug-resistant non-small cell lung cancer cell line A549 was at least as high as in the broadly chemosensitive ovarian teratocarcinoma cell line CH1(PA-1). (C) 2015 Elsevier Inc. All rights reserved.
机译:合成并表征了第12组金属的四个新配合物[Zn(II),Cd(II)和Hg(II)],以及结合在配体N-羟乙基-N-苯并咪唑基甲基乙二胺二乙酸上的钒基。通过X射线结构分析确定了具有Zn(II),Hg(II)和V(IV)的配合物的结构。在所有观察到的情况下,发现这些络合物的对称性是扭曲的八面体。证明了钒(IV)配合物对蛋白酪氨酸磷酸酶1B的抑制作用。钒(IV)复合物的细胞毒性在体外针对三种癌细胞进行了测试,并比较了游离配体以及乙酰丙酮氧钒和原钒酸钠的活性。该复合物的IC 50值在9至21μM的范围内。显着地,在多药耐药的非小细胞肺癌细胞系A549中的细胞毒性效力至少与对化学敏感的卵巢畸胎瘤细胞系CH1中的细胞毒性一样高。 (PA-1)。 (C)2015 Elsevier Inc.保留所有权利。

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