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

Chem Commun (Camb). 2024 Oct 8;60(81):11520-11523. doi: 10.1039/d4cc03106g.

Abstract

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 (IC50 MRC-5/T. brucei) of 2285-fold. We also correlate the impact of small structural changes to G4 binding activity and antiparasitic activity.

MeSH terms

  • Antiparasitic Agents / chemistry
  • Antiparasitic Agents / pharmacology
  • Azo Compounds* / chemistry
  • Azo Compounds* / pharmacology
  • Binding Sites
  • Drug Design*
  • G-Quadruplexes* / drug effects
  • Humans
  • Ligands
  • Molecular Structure
  • Trypanosoma brucei brucei* / drug effects

Substances

  • Ligands
  • Azo Compounds
  • azobenzene
  • Antiparasitic Agents