Interaction of novel dinuclear platinum and iron complexes with double strand DNA

1)合成了四个含氟或非取代苯基的五齿铁(II)配合物，并在过氧化氢存在下评价了它们对pUC19 DNA的切割活性。1)合成了1，8-(N-苯甲酰甲基)-双(N‘，N’-联吡啶甲基-R，R-环己烷-1，2-二胺)，1，在空气中抗坏血酸钠存在下评价了1，8-(N-蒽甲基)-双(N‘，N’-联吡啶-R，R-环己烷-1，2-二胺)对DNA的切割活性。1)合成了新的双核铂(II)配合物1，3-和1，4-(benzenedimethanethiolate-S)di(2，2‘，2“-terpyridine)platinum(II)氯化物四水合物(2和3)，研究了铂(II)配合物与小牛胸腺DNA的结合作用。配合物2与脱氧核糖核酸以插层方式发生强烈的相互作用，与之相比，化合物2为方形平面配合物，式为[Pt(L_2)(L_1)]X_2，其中L_1为S-2-氨基甲基吡咯烷或2-氨基甲基哌啶，L_2为二胺，合成了环丁烷-1，1-二羧基或1，10-菲咯啉，并用~1H核磁共振谱和X-射线晶体分析了L_1的配位性质。这些2-氨基甲基氮杂环烷衍生物形成五元螯合环，与顺或反构型的氮杂环烷环缩合。

In this project, I have aimed at the creation of various binuclear metal complexes such as Fe and Pt capable of cleaving and intercalating DNA.1-1)Four pentadentate iron(II) complexes containing non-or fluoro-substituted phenyl group were synthesized and cleaving activity of them to pUC19 DNA was evaluated in the presence of hydrogen peroxide. DNA cleavage activity increased with the number of substituted fluorine atoms on the phenyl group.1-2)I have synthesized 1,8-(N-anthranylmethyl)-bis(N',N'-dipyridylmethyl-R,R-cyclohexane-1,2-diamine), 1, and cleaving activity of 1 to DNA was evaluated in the presence of sodium ascorbate under air. A novel Fe complex 1 and sodium ascorbate system cleaved A-T rich region of DNA.2-1)The new dinuclear platinum(II) complexes, 1,3-and 1,4-(benzenedimethanethiolate-S)di(2,2',2"-terpyridine)platinum(II) chloride tetrahydrate (2 and 3), were synthesized in order to investigate the binding of platinum(II) complexes with calf thymus DNA, which was examined by UV and CD sepctroscopies. Complex 2 interacted strongly with DNA by intercalation compared to 3.2-2)Square-planar complex with the formula [Pt(L_2)(L_1)]X_2, where L_1 is S-2-aminomethylpyrrolidine or 2-aminomethylpiperidine and L_2 is diammine, cyclobutane-1,1-dicarboxylato or 1,10-phenanthroline were prepared and the nature of the coordination of L_1 was examined by ^1H NMR spectroscopy and X-ray crystallography. These 2-aminomethylazacycloalkane derivatives form five-membered chelate rings condensed with an azacycloalkane ring in cis or trans-configurations.