DNA polyintercalating drugs: DNA binding of diacridine derivatives.

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.