Two-ring DNA minor-groove binders consisting of readily available, di-substituted benzene derivatives

Article abstract of DOI:10.1016/S0960-894X(97)00244-8

DNA minor-groove binders consisting of two disubstituted benzene rings were prepared. Two ligands showed sequence selectivities higher than some of the best known minor-groove binders containing six-membered rings. Reversing the orientation of amide linkages in one ligand leads to another one with relaxed binding to AT sequences and greatly increased affinity toward GC sequences.