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不对称氧化钒配合物的合成与表征:DNA 结合、断裂研究及抗肿瘤活性。

Synthesis and characterization of unsymmetrical oxidovanadium complexes: DNA-binding, cleavage studies and antitumor activities.

机构信息

School of Pharmacy, Guangdong Pharmaceutical University, Guangzhou, 510006, People's Republic of China.

出版信息

J Inorg Biochem. 2012 Jul;112:39-48. doi: 10.1016/j.jinorgbio.2012.02.034. Epub 2012 Mar 13.

Abstract

Four oxidovanadium(IV) complexes, [VO(hntdtsc)(phen)] (1), [VO(hntdtsc)(bpy)] (2) (hntdtsc=2-hydroxy-1-naphthaldehyde thiosemicarbazone, phen=1,10-phenanthroline), [VO(satsc)(phen)] (3) and [VO(satsc)(bpy)] (4) (satsc=salicylaldehyde thiosemicarbazone, bpy=2,2'-bipyridine) have been synthesized and characterized. The results show that complexes 1, 2, 3 and 4 interact with DNA through intercalative mode and can efficiently cleave the plasmid pBR 322 DNA. It is interesting to note that these four complexes present highly cytotoxic activities against Myeloma cell (Ag8.653) and Gliomas cell (U251) lines. Complex 1 was found to be the most potent antitumor agent among the four complexes.

摘要

四种氧化钒(IV)配合物,[VO(hntdtsc)(phen)](1)、[VO(hntdtsc)(bpy)](2)(hntdtsc=2-羟基-1-萘醛缩硫代氨基脲,phen=1,10-菲咯啉)、[VO(satsc)(phen)](3)和[VO(satsc)(bpy)](4)(satsc=水杨醛缩硫代氨基脲,bpy=2,2'-联吡啶)已被合成并进行了表征。结果表明,配合物 1、2、3 和 4 通过嵌入模式与 DNA 相互作用,并能有效地切割质粒 pBR 322 DNA。有趣的是,这四种配合物对骨髓瘤细胞(Ag8.653)和神经胶质瘤细胞(U251)系具有高度的细胞毒性活性。配合物 1 被发现是这四种配合物中最有效的抗肿瘤剂。

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