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

Javier Ramos-Soriano; Maisie Holbrow-Wilshaw; Eliza Hunt; Y. Jennifer Jiang; Pablo Peñalver; Juan C. Morales; M. Carmen Galan

doi:10.1039/D4CC03106G

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

Javier Ramos-Soriano,

‡*^a Maisie Holbrow-Wilshaw,^a Eliza Hunt,^a Y. Jennifer Jiang,^a Pablo Peñalver,^b Juan C. Morales

*^b and M. Carmen Galan

*^a

Author affiliations

* Corresponding authors

^a School of Chemistry, Cantock's Close, University of Bristol, UK

^b Instituto de Parasitología y Biomedicina López Neyra, CSIC, PTS Granada, Avenida del Conocimiento, 17, Armilla, Granada, Spain
E-mail: fj.ramos@iiq.csic.es, jcmorales@ipb.csic.es, m.c.galan@bristol.ac.uk

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.

This article is part of the themed collection: ChemComm 60th Anniversary Collection

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DOI: https://doi.org/10.1039/D4CC03106G
Article type: Communication
Submitted: 25 jun 2024
Accepted: 10 sep 2024
First published: 13 sep 2024
This article is Open Access

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Chem. Commun., 2024,60, 11520-11523

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

J. Ramos-Soriano, M. Holbrow-Wilshaw, E. Hunt, Y. J. Jiang, P. Peñalver, J. C. Morales and M. C. Galan, Chem. Commun., 2024, 60, 11520 DOI: 10.1039/D4CC03106G

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

Abstract

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

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