SYNTHESIS AND PROPERTIES OF OLIGONUCLEOTIDES COVALENTLY-LINKED TO INTERCALATING AGENTS

The chemical precesses involved in the preparation of oligonucleotide- intercalator conjugates are reviewed. Two strategies are used to coval ently attach an intercalating agent to oligonucleotides; it can be eit her directly incorporated during the oligonucleotide chain assembly or linked to the unblocked oligonucleotide using a specific coupling rea ction. The covalent attachment of different intercalating agents to va rious positions of an oligonucleotide chain: 5'-, 3'-, both 5'- and 3' -ends, internucleotidic phosphate, 1'- or 2'-position of a sugar resid ue or nucleic base is reported, Studies of the binding of these modifi ed oligonucleotides to their targets are also presented together with some of the unique properties which are conferred upon the oligonuleot ides by attachment of an intercalating agent.