FRET-based DNA thermal denaturation assay results (ΔTm values) for the interaction of the PBD monomers (1–5) and dimers (6–8) (Figure 1) with eight different G-quadruplex-forming DNA sequences and a duplex DNA control (Table 1).

KMR-04-12 (11, Figure 3) was included as a positive quadruplex-binding control molecule, and the MPB-Py-Py fragment 12 (Figure 3) was evaluated to represent the isolated C8-substituent of the PBD C8-Conjugate 5 (Figure 1).aESDS±0.5°CbConcentration of DNA was 1 µM in these experiments; in all other cases it was 200 nM. Differences in ΔTm values for duplex DNA at the highest ligand concentration of 50 µM (50∶1, ligand:G4) are thought to be due to solubility or aggregation issues at these artificially high concentrations of ligand and DNA.