Synthesis of Oligonucleotide-Intercalator Conjugates Capable to Inhibit HIV-1 DNA Integration

Abstract This investigation is devoted to design of short “switch” oligonucleotides mono- or bi-functionnalized with intercalating agents capable to form a stable triplex with HIV integrase-cognate sequences and inhibit selectively HIV integration. Methods of intercalator incorporation at 5′- and/or 3′-terminal positions or one of the pyrimidine heterocyclic bases are developed.