New DNA minor-groove binding molecules with high sequence-selectivities and binding affinities.

New DNA minor-groove binding molecules with high binding affinities and sequence-selectivities are described. The effects of structural changes in ligands with a three-ring backbone on their DNA-binding properties have been studied. Of a pool of eight potential ligands, two showed binding affinities and sequence-selectivities rivaling distamycin. The two best ligands share a common structural motif that involves a para-di-substituted benzene ring flanked by two meta-di-substituted benzene rings.