SYNTHESIS OF PURINE-ACRIDINE HYBRID MOLECULES RELATED TO ARTIFICIAL ENDONUCLEASES

In the course of a program devoted to the synthesis of artificial endonucleases, we have previously reported a series of hybrid molecules in which a purine is linked to an intercalating drug by a polyamino chain. These molecules recognize and cleave selectively abasic sites in DNA with very high efficiency. In order to get insight into the mechanism of recognition and cleavage, we have prepared a new series of molecules in which the purine is linked to an amino-acridine by an aliphatic chain containing amido or/and amino groups. The key intermediates are alpha-halo-omega-amino polyaza chains which may be of general use as linkers in bioconjugate chemistry.