新型双核芳基钌配合物的合成、结构、抗癌活性及与DNA相互作用研究

Novel dinuclear arene ruthenium(Ⅱ) complexes:synthesis,structure,anticancer activity and interaction with DNA

本文使用柔性配体1,3-二(1-咪唑-亚甲基)-2,4,6-三甲基苯(m-bitmb)与对甲基异丙基芳基钌反应,合成了两种新型的M_2L_2双核环状芳基钌配合物[{Ru(η~6-p-cymene)}_2(m-bitmb)_2Cl_2](SbF_6)_2(1)和[{Ru(η~6-p-cymene)}_2(m-bitmb)_2Cl_2](CF_3COO)_2(2),通过单晶衍射、核磁共振波谱、质谱和元素分析等方法表-征了它们的结构,并用3-(4,5-二甲基噻唑-2)2,5-二苯基四氮唑溴盐(MTT)法、圆二色谱和琼脂糖凝胶电泳等方法研究了抗癌活性及其与DNA的相互作用.结果表明,两个配合物具有"椅式"构型;均具有一定的抗癌活性,其中2对HeLa细胞株有较强的杀伤作用;均可使CT-DNA、PBR322质粒DNA的构象发生变化,且2与DNA的作用较强,这与其抗癌活性结果相一致.

Two new dinuclear Ru（Ⅱ） arene M2L2 metallocycle complexes[Ru2（η^6-p-cymene）2（m-bitmb）2Cl2]（SbF6）2（1）and[Ru2（η^6-p-cymene）2（m-bitmb）2Cl2]（CF3COO）2（2）（m-bitmb=1,3-bis（imidazol-l-ymethyl）-2,4,6-trimethylbenzene）were synthesized and characterized by single crystal X-ray diffraction,-1H NMR,ESI-MS and elemental analysis.Results revealed that complex 1 and 2 are M2L2 dinuclear Ru-arene complexes with unique ＂chair-like＂ conformation.Both of complexes 1 and 2 had certain anti-cancer activity,and complex 2 performed good cytotoxic effect on HeLa cells.The results of circular dichroism and agarose gel electrophoresis experiments indicated that complexes 1 and 2could change the conformation of CT-DNA and PRB322 DNA.Moreover,compared with 1,2 presented much stronger interaction with DNA,which was in accordance with their anti-cancer activities.