SYNTHESIS OF PURINE-ACRIDINE HYBRID MOLECULES RELATED TO ARTIFICIAL ENDONUCLEASES

In the course of a program devoted to the synthesis of artificial endo nucleases, we have previously reported a series of hybrid molecules in which a purine is linked to an intercalating drug by a polyamino chai n. These molecules recognize and cleave selectively abasic sites in DN A with very high efficiency. In order to get insight into the mechanis m of recognition and cleavage, we have prepared a new series of molecu les 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.