论文部分内容阅读
本文合成了三种铂髤配合物PtLCl(HL1=2-(3′,5′-二甲基-吡唑-1′-基)-N-(2″-吡啶甲基)乙基胺;HL2=2-(3′,5′-二甲基-吡唑-1′-基)-N-(2″-吡啶乙基)乙基胺;HL3=2-(3′,5′-二甲基-吡唑-1′-基)-N-(喹啉-8″-基)乙基胺,通过元素分析和质谱进行结构表征。利用荧光和圆二色光谱研究了3种配合物与小牛胸腺DNA的相互作用,结果发现配体结构对配合物与DNA的作用方式及强度产生极大影响。PtL3Cl具有较大的共轭平面而易以嵌入模式与DNA结合,而PtL1Cl和PtL2Cl的空间位阻较小,易与DNA以共价模式结合。通过质谱跟踪发现,配合物PtL1Cl和PtL2Cl均能与5′-鸟苷酸(5′-GMP)发生共价结合,但是没有发现PtL3Cl与5′-GMP的加合物。3种配合物对人宫颈癌细胞的体外毒活性数据表明:PtL3Cl的细胞毒活性最强。
In this paper, three kinds of Pt l complexes PtLCl (HL1 = 2- (3 ’, 5’-dimethyl-pyrazol-1’- = 2- (3 ’, 5’-dimethyl-pyrazol- 1’-yl) -N- (2 “-pyridylethyl) ethylamine; HL3 = 2- Pyrazol-1’-yl) -N- (quinoline-8 ”-yl) ethylamine, and its structure was characterized by elemental analysis and mass spectrometry. The fluorescence spectra and circular dichroism The interaction between bovine thymus DNA and the results showed that the ligand structure had a great influence on the mode of action and the strength of the complexes with DNA.PtL3Cl has a large conjugate plane and is easy to embed DNA binding patterns, while the space of PtL1Cl and PtL2Cl The results showed that both PtL1Cl and PtL2Cl could covalently bind with 5’-GMP, but PtL3Cl and 5 ’-GMP adduct.The in vitro cytotoxic activity of the three complexes on human cervical cancer cells showed that PtL3Cl had the strongest cytotoxic activity.