In this review, drug oligonucleotide conjugates synthesized and characterized in our laboratories will be discussed. An idealized view of a complex between an acridine-oligonucleotide conjugate and RNA is shown above. In addition, other related conjugates will be reviewed. The goal of this review is to establish that it is now feasible to synthesize a wide range of drug oligonucleotide conjugates. The testing of these molecules will provide important information on the pharmacological usefulness of targeting drugs to specific sequences using oligonucleotides.