NEW DNA MINOR-GROOVE BINDING-MOLECULES WITH HIGH SEQUENCE-SELECTIVITIES AND BINDING AFFINITIES

New DNA minor-groove binding molecules with high binding affinities an d sequence-selectivities are described. The effects of structural chan ges in ligands with a three-ring backbone on their DNA-binding propert ies have been studied. Of a pool of eight potential ligands, two showe d binding affinities and sequence-selectivities rivaling distamycin. T he two best ligands share a common structural motif that involves a pa ra-di-substituted benzene ring flanked by two meta-di-substituted benz ene rings. (C) 1997 Academic Press.