Probing the binding and antiparasitic efficacy of azobenzene G-quadruplex ligands to investigate G4 ligand design.

Novel strategies against parasitic infections are of great importance. Here, we describe a G4 DNA ligand with subnanomolar antiparasitic activity against T. brucei and a remarkable selectivity index (IC 50 MRC-5/ T. brucei ) of 2285-fold. We also correlate the impact of small structural changes to G4 binding activity and antiparasitic activity.