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设计、结构解析、DNA 结合、切割、自由基清除活性和 5-二甲基-2-苯基-4-[(吡啶-2-基亚甲基)氨基]-1,2-二氢-吡唑-3-酮席夫碱配体与铜(I)配合物的比较。

Designing, structural elucidation, comparison of DNA binding, cleavage, radical scavenging activity and anticancer activity of copper(I) complex with 5-dimethyl-2-phenyl-4-[(pyridin-2-ylmethylene)-amino]-1,2-dihydro-pyrazol-3-one Schiff base ligand.

机构信息

Post Graduate and Research Department of Chemistry, Sri Ramakrishna Mission Vidyalaya College of Arts and Science, Coimbatore 641 020, Tamil Nadu, India.

出版信息

Eur J Med Chem. 2013 Jun;64:81-9. doi: 10.1016/j.ejmech.2013.03.047. Epub 2013 Apr 6.

Abstract

A novel copper(I) Schiff base complex has been synthesized and fully characterized by spectral, analytical and structural modes. Single crystal X-ray diffraction studies revealed that the copper(I) complex [CuCl(PPh3)L] has a distorted tetrahedral geometry around the central copper(I) ion. The interaction of the ligand and the complex with CT-DNA has been explored by absorption titration method which revealed that the compounds could interact with CT-DNA through intercalation. A gel electrophoresis assay demonstrated the ability of the complex to cleave the pBR322 DNA. The antioxidative properties showed that the copper(I) complex has a strong radical-scavenging potency than ligands. Further the cytotoxic effect of the compounds examined on cancerous cell lines showed that the complex exhibited substantial anticancer activity.

摘要

一种新型的铜(I)希夫碱配合物已经通过光谱、分析和结构模式被合成并进行了充分的表征。单晶 X 射线衍射研究表明,铜(I)配合物 [CuCl(PPh3)L] 具有扭曲的四面体几何形状,其中中心铜(I)离子位于其中心。通过吸收滴定法研究了配体和配合物与 CT-DNA 的相互作用,该方法表明化合物可以通过嵌入与 CT-DNA 相互作用。凝胶电泳实验证明了该配合物具有切割 pBR322 DNA 的能力。抗氧化性能表明,铜(I)配合物具有比配体更强的自由基清除能力。进一步研究了化合物对癌细胞系的细胞毒性作用,结果表明该配合物具有显著的抗癌活性。

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