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含有对称双膦桥联配体的钯环配合物的体外细胞毒性研究。研究它们与 DNA 和 BSA 的相互作用。

In vitro cytotoxicity studies of palladacyclic complexes containing the symmetric diphosphine bridging ligand. Studies of their interactions with DNA and BSA.

机构信息

Department of Chemistry, Isfahan University of Technology, Isfahan 84156/83111, Iran.

Department of Pharmaceutical Chemistry, Isfahan University of Medical Sciences, Isfahan, Iran.

出版信息

Eur J Med Chem. 2014 Feb 12;73:8-17. doi: 10.1016/j.ejmech.2013.11.042. Epub 2013 Dec 12.

Abstract

The reactions between [Pd2{(C,N)-C6H4CH2NH(Et)}2(μ-X)2] (X = Cl or Br) and 1,2-bis(diphenylphosphino)ethane (dppe) in the 1:1 molar ratio resulted in the dppe-bridged Pd(II) complexes, [Pd2{(C,N)-C6H4CH2NH(Et)}2(μ-dppe)(Cl)2] (1) and [Pd2{(C,N)-C6H4CH2NH(Et)}2(μ-dppe)(Br)2] (2), respectively, which were characterized by elemental analyses, infrared (IR), (1)H- and (31)P{(1)H} NMR spectroscopy. The molecular structure of 1 was determined by single-crystal X-ray diffraction. In vitro cytotoxicity of 1, 2, dppe, PhCH2NH(Et) and cisplatin were carried out against four human tumor cell lines. The interactions of complexes towards DNA and protein are investigated. The results suggested that both complexes could interact with FS-DNA through the intercalation mode. Moreover, the reactivity towards BSA revealed that the microenvironment and the secondary structure of BSA were changed in the presence of Pd(II) complexes.

摘要

反应之间 [Pd2{(C,N)-C6H4CH2NH(Et)}2(μ-X)2](X = Cl 或 Br)和 1,2-双(二苯基膦)乙烷(dppe)在 1:1 摩尔比下得到 dppe 桥联 Pd(II)配合物,[Pd2{(C,N)-C6H4CH2NH(Et)}2(μ-dppe)(Cl)2](1)和[Pd2{(C,N)-C6H4CH2NH(Et)}2(μ-dppe)(Br)2](2),分别通过元素分析、红外(IR)、(1)H-和(31)P{(1)H} NMR 光谱进行了表征。1 的分子结构通过单晶 X 射线衍射确定。对 1、2、dppe、PhCH2NH(Et)和顺铂进行了四种人肿瘤细胞系的体外细胞毒性试验。研究了配合物与 DNA 和蛋白质的相互作用。结果表明,两种配合物都可以通过嵌入模式与 FS-DNA 相互作用。此外,对 BSA 的反应性表明,Pd(II)配合物的存在改变了 BSA 的微环境和二级结构。

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