Department of Chemistry, State University of New York at Geneseo, 1 College Circle, Geneseo, NY 14454, USA.
Bioorg Med Chem Lett. 2011 Jul 15;21(14):4288-91. doi: 10.1016/j.bmcl.2011.05.069. Epub 2011 May 25.
A combination of isothermal titration calorimetry (ITC), topoisomerase I DNA unwinding assays, and ethidium bromide displacement studies were employed to investigate the binding of a homologous series of naphthalene diimides (NDI) to DNA. Our results suggest that the nature of the substituent plays a significant role in both the preferred binding mode and relative binding affinity of the compounds of this study. Only intercalative-type binding (K=15±3×10(6)M(-1)) was observed for the NDI with the smallest substituent (trimethyl-ethylamino), while larger members of the series (diethylmethyl-, dipropylmethyl- and dibutylmethyl-ethylamino substituents) adopted an additional binding mode of higher affinity (K(1)=31-78×10(6)M(-1)).
采用等温滴定量热法（ITC）、拓扑异构酶 I DNA 解旋测定法和溴化乙锭置换研究相结合的方法，研究了一系列萘二酰亚胺（NDI）同系物与 DNA 的结合。我们的结果表明，取代基的性质在本研究化合物的首选结合模式和相对结合亲和力中都起着重要作用。只有取代基最小的 NDI（三甲基乙基氨基）表现出嵌入型结合（K=15±3×10(6)M(-1)），而该系列的较大成员（二乙基甲基-、二丙基甲基-和二丁基甲基-乙基氨基取代基）采用了具有更高亲和力的附加结合模式（K(1)=31-78×10(6)M(-1)）。
