ABSTRACT A new family of conjugates between the Hoechst minor groove binder and the TACN metal ion ligand connected through hydrophobic alkyl or more hydrophilic oxyethyl linkers of different length has been prepared. The linkers are connected to the convex side of the Hoechst skeleton thus forcing the TACN ligand to exit the minor groove and interact with the phosphate backbone of DNA. The conjugates preserve the binding mode of Hoechst with an affinity influenced by the nature of the linker, the more hydrophobic being the more efficient. Coordination of Cu(II) or Zn(II) poorly affect these parameters. Nevertheless, the Zn(II) complex bearing a C6 linear alkyl linker induced a modest but reproducible acceleration of the hydrolytic cleavage of DNA which can be ascribed to the ability of the conjugate to deliver the hydrolytic subunit close to the DNA phosphodiester bonds. GRAPHICAL ABSTRACT

中文翻译：

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与 Hoechst-TACN 偶联物的质粒 DNA 的相互作用

摘要 Hoechst 小沟结合剂和 TACN 金属离子配体通过不同长度的疏水性烷基或更亲水性氧乙基连接体连接的新型偶联物家族已被制备。接头连接到 Hoechst 骨架的凸面，从而迫使 TACN 配体退出小沟并与 DNA 的磷酸骨架相互作用。偶联物保留了 Hoechst 的结合模式，其亲和力受接头性质的影响，疏水性越强，效率越高。Cu(II) 或 Zn(II) 的配位对这些参数影响很小。尽管如此，带有 C6 线性烷基接头的 Zn(II) 复合物诱导了 DNA 水解裂解的适度但可重复的加速，这可以归因于缀合物将水解亚基传递到 DNA 磷酸二酯键附近的能力。图形概要