靶向DNA的刚性配体的双核芳基钌配合物（英文）  

DNA Targeting Rigid Dinuclear Ruthenium-Arene Complexes

作　　者：李季[1] 郝元元 钱勇[1] 薛旭玲 苏志 刘红科[1,2] LI Ji;HAO Yuan-Yuan;QIAN Yong;XUE Xu-Lin;SU Zhi;LIU Hong-Ke(College of Chemistry and Materials Science,Jiangsu Key Laboratory of Biofunctional Materials,Nanjing Normal University,Nanjing 210023,China;State Key Laboratory of Coordination Chemistry,School of Chemistry and Chemical Engineering,Nanjing University,Nanjing 210023,China)

机构地区：[1]南京师范大学化学与材料科学学院,江苏生物功能材料重点实验室,南京210023 [2]南京大学化学化工学院,配位化学国家重点实验室,南京210023

出　　处：《无机化学学报》2019年第8期1500-1508,共9页Chinese Journal of Inorganic Chemistry

基　　金：国家自然科学基金国际合作重点项目(No.21420102002);国家自然基金(No.21601088,21771109,21778033);江苏省自然科学基金(No.BK20171472)资助

摘　　要：以刚性配体1,3-bib(1,3-二(1H-咪唑-1-基)苯)与[Ru(η^6-p-bip)Cl2]2( p-bip,联苯基团)为原料,合成了3种双核芳基钌配合物[Ru2(η^6-p-bip)2(1,3-bib)2XY]X2(X=Y=Cl^-(1),X=Y=Br^-(2),X=I^-和Y=Cl^-(3),并用核磁和质谱等对配合物进行了表征。配合物1的单晶衍射结果表明其具有一种刚性双核M2L2碗状结构,空腔中心有一个阴离子Cl^-。配合物3对A549细胞有较高的抗癌活性(IC50=13.9 μmol·L^-1),与顺铂细胞毒性(IC50=15.2 μmol·L^-1)相当。紫外吸收光谱、圆二色谱、凝胶电泳法研究表明配合物1~3与DNA发生强烈的相互作用并且诱发DNA发生解旋。Three dinuclear Ru(Ⅱ)-arene complexes [Ru2(η^6-p-bip)2(1,3-bib)2XY]X2 (X=Y=Cl^-(1),X=Y=Br^-(2),X=I^- and Y=Cl^-(3);1,3-bib=1,3-di(1H-imidazol-1-yl)benzene,p-bip=biphenyl) were synthesized and fully characterized by 1H NMR and ESI-MS.Single crystal X-ray diffractions studies showed that complex 1 owns a rigid M2L2 bowl-like structure,where one Cl^- is trapped inside the cavity to balance the charge.Complex 3 showed the best anticancer activities among complexes 1~3.The IC50 value of 3 towards to human lung cancer cells (A549) reached to 13.9 μmol·L^-1,which is comparable to that of cisplatin (IC50=15.2 μmol·L^-1).Complexes 1~3 have shown strong interactions with DNA and could induce the unwinding of the DNA superhelix structure.CCDC: 1875666,1.

关 键 词：芳基钉 晶体结构 抗癌活性 DNA作用 

分 类 号：O614.821[理学—无机化学]