为开发新型钌(Ru)抗肿瘤药物,以3-甲基-2-噻吩甲醛-4-羟基苯甲酰肼席夫碱配体(L)合成了[Ru(L)(DMSO)2Cl2](1)(DMSO=二甲基亚砜).用X射线单晶衍射法测定了1的晶体结构.配合物1的结构由1个Ru(Ⅱ)中心离子与2个DMSO分子、2个氯离子、1个L配位而成.通过MTT实验分析,1对T24细胞表现出良好的抗肿瘤活性.同时,通过彗星实验、蛋白质印迹实验和DNA琼脂糖凝胶电泳实验结果证明1可以有效结合DNA,诱导DNA损伤,最终杀死肿瘤细胞.导致DNA损伤的原因很可能是由于细胞与1孵育后细胞内可以产生大量的活性氧.
To develop a novel antitumor Ru agent, [Ru(L) (DMSO)2Cl2] (1) (DMSO=dimethyl sulfoxide) was synthe-sized by employing a Schiff base ligand 3-methyl-2-thiophenecarboxaldehyde-4-hydroxybenzhydrazide (L). The sin-gle crystal X-ray crystallographic study was carried out to determine the crystallographic structure of 1. The struc-ture of complex 1 is composed of a central Ru(Ⅱ) ion, two DMSO molecules, two chloride ions, and a ligand L. In addition, 1 possessed strong antitumor activity against T24 cells by MTT analysis. Furthermore, the potential antitu-mor mechanism of 1 was investigated by comet assays, western-blotting assays, and DNA agarose gel electrophore-sis. These results indicate that 1 can effectively bind to DNA and induce DNA damage, and eventually kill the tumor cells. DNA damage may be caused by the production of reactive oxygen species. CCDC:2080249.