ABSTRACT Progress in the development of DNA sequence selective minor groove binding agents is discussed. Among the factors contributing to the molecular recongnition process are: the presence and disposition of hydrogen bond accepting and donating groups, ligand shape, chirality, stereochemistry, flexibility, and charge. For longer ligands the critical features is the application of these factors in the design and synthesis of novel agents which exhibit potent anticancer, and antiviral properties and inhibition of critical cellular enzymes including topoisomerases and, in the case of viruses, of reverse transcriptase is discussed. The emerging evidence of a relationship between sequence selectivity of the new agents and the biological responses they invoke is also described.
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