Increase in the apparent intercalation ability of a platinum complex via multivalency by installation into the sidechain of a graft copolymer and observation of structural changes in the intercalated DNA

Metal complexes with planar structures have been utilized as DNA intercalators that can be inserted into the base pairs of DNA strands, and have potential applications in DNA-targeting drug therapies. When designing the intercalator metal complexes, controlling their interactions with DNA is important, and has been performed by modifying the chemical structure of the metal ligand. Herein, we designed a graft copolymer segment having Pt complexes with bipyridine and poly(ethylene glycol) (p(PEGMA-co-BPyMA-Pt)) as another strategy to control the interaction with DNA via a multivalent effect. The p(PEGMA-co-BPyMA-Pt) increased not only the binding constant as one macromolecule but also the apparent binding constant per intercalator unit compared to the Pt complex with bipyridine (BPy-Pt). Moreover, p(PEGMA-co-BPyMA-Pt) induced a larger change in DNA structure using lower amounts of Pt than BPy-Pt. These observed properties of p(PEGMA-co-BPyMA-Pt) suggest that grafting intercalators on polymer segments is a promising approach for designing novel types of intercalators.