The synthesis and characterization of a small series of cyclic triimidazole derivatives functionalized with methylated pyridine or guanidine moieties is reported. These compounds were tested for their ability to bind to G-quadruplexes from both telomeric and oncogene promoter sequences. Some of them exhibited high affinity and effective G-quadruplex-stabilizing properties. Overall, these compounds may represent useful leads for developing more potent and selective analogues

Cyclic Triimidazoles as Stabilizers for Gene Promoter and Human Telomeric DNA G‐Quadruplexes / D. Malpicci, S. Andolina, S. Di Ciolo, E. Lucenti, E. Cariati, S. Marzano, B. Pagano, J. Amato, A. Randazzo, C. Giannini. - In: EUROPEAN JOURNAL OF ORGANIC CHEMISTRY. - ISSN 1434-193X. - 2022:35(2022 Sep 20), pp. e202200718.1-e202200718.9. [10.1002/ejoc.202200718]

Cyclic Triimidazoles as Stabilizers for Gene Promoter and Human Telomeric DNA G‐Quadruplexes

D. Malpicci
Primo
;
E. Lucenti;E. Cariati;C. Giannini
Ultimo
2022

Abstract

The synthesis and characterization of a small series of cyclic triimidazole derivatives functionalized with methylated pyridine or guanidine moieties is reported. These compounds were tested for their ability to bind to G-quadruplexes from both telomeric and oncogene promoter sequences. Some of them exhibited high affinity and effective G-quadruplex-stabilizing properties. Overall, these compounds may represent useful leads for developing more potent and selective analogues
Aminoguanidine; Cyclic triimidazole; G-quadruplex; Ligand design; N-methylated pyridine;
Settore CHIM/06 - Chimica Organica
PSRL220LPRAT_01 - Piano di Sostegno alla Ricerca 2015-2017 - Linea 2 "Dotazione annuale per attività istituzionali" (anno 2020) - PRATI, LAURA - PSR_LINEA2_ / Piano di sviluppo di ricerca - Dotazioni dipartimentali - Linea 2 - 2020
8-ago-2022
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/2434/938346
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