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

Autor: Ramos-Soriano J; School of Chemistry, Cantock's Close, University of Bristol, BS8 1TS, UK., Holbrow-Wilshaw M; School of Chemistry, Cantock's Close, University of Bristol, BS8 1TS, UK., Hunt E; School of Chemistry, Cantock's Close, University of Bristol, BS8 1TS, UK., Jiang YJ; School of Chemistry, Cantock's Close, University of Bristol, BS8 1TS, UK., Peñalver P; Instituto de Parasitología y Biomedicina López Neyra, CSIC, PTS Granada, Avenida del Conocimiento, 17, 18016, Armilla, Granada, Spain. fj.ramos@iiq.csic.es., Morales JC; Instituto de Parasitología y Biomedicina López Neyra, CSIC, PTS Granada, Avenida del Conocimiento, 17, 18016, Armilla, Granada, Spain. fj.ramos@iiq.csic.es., Galan MC; School of Chemistry, Cantock's Close, University of Bristol, BS8 1TS, UK.
Jazyk: angličtina
Zdroj: Chemical communications (Cambridge, England) [Chem Commun (Camb)] 2024 Oct 08; Vol. 60 (81), pp. 11520-11523. Date of Electronic Publication: 2024 Oct 08.
DOI: 10.1039/d4cc03106g
Abstrakt: 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.
Databáze: MEDLINE