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合成、表征及具有改良联吡啶和联吡啶胺配体的金（III）化合物的生物性质。

Synthesis, characterisation and biological properties of gold(III) compounds with modified bipyridine and bipyridylamine ligands.

机构信息

Institut des Sciences et Ingénierie Chimiques, Ecole Polytechnique Fédérale de Lausanne (EPFL), CH-1015 Lausanne, Switzerland.

出版信息

Dalton Trans. 2010 Mar 7;39(9):2239-45. doi: 10.1039/b921019a. Epub 2010 Jan 7.

DOI:10.1039/b921019a
PMID:20162197
Abstract

Square planar gold(III) complexes that contain functionalised bipyridine ligands of general formula [Au(N--N)Cl(2)][PF(6)] [where N--N = 2,2'-bipyridine, 4,4'-dimethyl-2,2'-bipyridine, 4,4'-dimethoxy-2,2'-bipyridine and 4,4'-diamino-2,2'-bipyridine] have been prepared and characterised by NMR spectroscopy and mass spectrometry. Two of the complexes have also been characterised in the solid state by X-ray crystallography. In addition, a gold(iii) compound bearing a dipyridin-2-ylamine ligand was also prepared and characterised. The complexes were found to undergo hydrolysis under pseudo-physiological conditions. Moreover, the complexes showed moderate to good cytotoxicity in vitro towards the A2780 human ovarian carcinoma cell line and the cisplatin resistant variant A2780cisR. Reactivity studies with biomolecules, such as reducing agents, plasmid DNA and a model protein (ubiquitin) were also performed to provide tentative insights into the mode of action of the complexes.

摘要

已制备并通过 NMR 光谱和质谱法对具有通用式[Au（N--N）Cl（2）][PF（6）]的功能化双吡啶配体的平面正方形金（III）配合物进行了表征[N--N=2,2'-联吡啶，4,4'-二甲基-2,2'-联吡啶，4,4'-二甲氧基-2,2'-联吡啶和 4,4'-二氨基-2,2'-联吡啶]。其中两个配合物也通过 X 射线晶体学在固态下进行了表征。此外，还制备并表征了一种带有二吡啶-2-基胺配体的金（III）化合物。这些配合物在类生理条件下会发生水解。此外，这些配合物对 A2780 人卵巢癌细胞系和顺铂耐药变体 A2780cisR 具有中等至良好的体外细胞毒性。还进行了与生物分子（例如还原剂，质粒 DNA 和模型蛋白（泛素）的反应性研究，以提供对配合物作用方式的初步了解。

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