Thioglycosides as vectors for G-quadruplex ligands: potent anticancer and antiparasitic drugs

Efres Belmonte-Reche; Filippo Doria; Marta Martínez-García; Michela Zuffo; Aurore Guedin; Adriana Stucchi; Jenny Campos-Salinas; María Cabello-Donayre; José María Pérez-Victoria; Jean Louis Mergny; Mauro Freccero; Juan Carlos Morales

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Thioglycosides as vectors for G-quadruplex ligands: potent anticancer and antiparasitic drugs

Efres Belmonte-Reche

¹,

Filippo Doria

¹,

Marta Martínez-García

¹,

Michela Zuffo

²,

Aurore Guedin

³,

Adriana Stucchi

¹,

Jenny Campos-Salinas

¹,

María Cabello-Donayre

¹,

José María Pérez-Victoria

¹,

Jean Louis Mergny

⁴,

Mauro Freccero

²,

Juan Carlos Morales

^{*

1}

¹ Department of Biochemistry and Molecular Pharmacology, Instituto de Parasitología y Biomedicina López Neyra, CSIC, PTS Granada, Avda. del Conocimiento, 17, 18016 Armilla, Granada, Spain
² Department of Chemistry, University of Pavia, V. le Taramelli 10, 27100 Pavia, Italy
³ ARNA Laboratory, Université de Bordeaux, Inserm U1212, CNRS UMR5320, Institut Européen de Chimie Biologie (IECB), 2 Rue Robert Escarpit, 33607 Pessac, France
⁴ Laboratoire d’optique et Biosciences, Ecole Polytechnique, Inserm U1182, CNRS UMR7645, Institut Polytechnique de Paris, Palaiseau, France

Academic Editor: Alfredo Berzal-Herranz

Published: 01 November 2023 by MDPI in 9th International Electronic Conference on Medicinal Chemistry session Invited lectures

https://doi.org/10.3390/ECMC2023-15562 (registering DOI)

Abstract:

G-quadruplexes (G4) are DNA secondary structures that play important roles in the regulation of gene expression in human cells and have been proposed as therapeutic targets in cancer. At the same time, putative G-quadruplex forming sequences have also been found on the genome of parasites T. brucei, L. major and P. falciparum suggesting they could also be explored as therapeutic targets.

We have designed and prepared thio sugars as vectors for naphthalene diimides, a classical G-quadruplex ligand, aiming to improve binding to G4 and biostability. Recent results on their efficacy against cancer cells and parasitic infections will be presented.

Keywords: /

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