Le Pecq J B, Le Bret M, Barbet J, Roques B
Proc Natl Acad Sci U S A. 1975 Aug;72(8):2915-9. doi: 10.1073/pnas.72.8.2915.
As a first step in the synthesis and the study of DNA polyintercalating drugs, dimers of acridines have been prepared. Their DNA binding properties have been studied. It has been determined that when the chain separating the two aromatic rings is longer than a criticål distance, bisintercalation is actually observed and that the DNA binding affinity becomes quite large (greater than 10(8)-10(9) M-1). It is shown also that the optical characteristics of these molecules are dependent on the sequences of DNA. The fluorescence intensity of one of these dimers when bound to DNA varies as the fourth power of its A+T content. This derivative could be used as a fluorescent probe of DNA sequence.
作为合成和研究DNA多嵌入药物的第一步，已制备了吖啶二聚体。对它们与DNA的结合特性进行了研究。已确定当分隔两个芳香环的链长于临界距离时，实际上会观察到双嵌入现象，并且DNA结合亲和力变得相当大（大于10⁸ - 10⁹ M⁻¹）。还表明这些分子的光学特性取决于DNA的序列。其中一种二聚体与DNA结合时的荧光强度随其A + T含量的四次方而变化。这种衍生物可用作DNA序列的荧光探针。
