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2-氧代-1,2-二氢苯并[h]喹啉-3-甲酰基缩氨硫脲单核钴(III)配合物的 DNA 结合、抗氧化和细胞毒性活性评价。

Evaluation of DNA binding, antioxidant and cytotoxic activity of mononuclear Co(III) complexes of 2-oxo-1,2-dihydrobenzo[h]quinoline-3-carbaldehyde thiosemicarbazones.

机构信息

Department of Chemistry, Bharathiar University, Coimbatore 641046, India.

出版信息

Eur J Med Chem. 2012 Apr;50:405-15. doi: 10.1016/j.ejmech.2012.02.026. Epub 2012 Feb 18.

Abstract

Four new 2-oxo-1,2-dihydrobenzo[h]quinoline-3-carbaldehyde N-substituted thiosemicarbazone ligands (H(2)-LR, where R = H, Me, Et or Ph) and their corresponding new cobalt(III) complexes have been synthesized and characterized. The structures of the complexes 2 and 3 were determined by single crystal X-ray diffraction analysis. The interactions of the new complexes with DNA were investigated by absorption, emission and viscosity studies which indicated that the complexes bind to DNA via intercalation. Antioxidant studies of the new complexes showed that the significant antioxidant activity against DPPH radical. In addition, the in vitro cytotoxicity of complexes 1-4 against A549 cell line was assayed which showed higher cytotoxic activity with lower IC(50) values indicating their efficiency in killing the cancer cells even at very low concentrations.

摘要

四种新的 2-氧代-1,2-二氢苯并[h]喹啉-3-甲酰基 N-取代缩氨基硫脲配体(H(2)-LR,其中 R = H、Me、Et 或 Ph)及其相应的新型钴(III)配合物已被合成和表征。配合物 2 和 3 的结构通过单晶 X 射线衍射分析确定。通过吸收、发射和粘度研究研究了新配合物与 DNA 的相互作用,表明配合物通过嵌入与 DNA 结合。新配合物的抗氧化研究表明,它们对 DPPH 自由基具有显著的抗氧化活性。此外,还测定了配合物 1-4 对 A549 细胞系的体外细胞毒性,结果表明,它们具有更高的细胞毒性,IC(50)值更低,这表明它们即使在非常低的浓度下也能有效地杀死癌细胞。

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