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

Malpicci;Daniele;Lucenti;Elena;Cariati;Elena;
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.
2022
Istituto di Scienze e Tecnologie Chimiche "Giulio Natta" - SCITEC
Aminoguanidine
Cyclic triimidazole
G-quadruplex
Ligand design
N-methylated pyridine
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/20.500.14243/416002
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