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New Ruthenium-based probes for selective G-quadruplex targeting.

par Piraux, Guillaume;Bar, Laure;Abraham, Michael M.H.;Lavergne, Thomas;Jamet, Hélène;Dejeu, Jérôme;Marcelis, Lionel ;Defrancq, Eric;Elias, Benjamin
Référence Chemistry
Publication Publié, 2017-06

Article révisé par les pairs

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Résumé :

Telomeric regions containing G-quadruplexes (G4s) structures play a pivotal role in the development of cancers. The development of specific binders for G4s is thus of great interest in order to get deeper understanding of the role of these structures, and to ultimately develop new anti-cancer drugs candidates. For several years, RuII complexes have been studied as efficient probe for DNA. Their main interest is the tunability of their structures and properties, and the possibility to use light excitation as a tool to probe the environment of these complexes or selectively trigger a reaction with a biological target. In this paper, we report on the synthesis and thorough study of new RuII complexes based on the novel dipyrazino[2,3-a:2',3'-h]phenazine ligand (dph), obtained via a Chichibanin-like reaction. Luminescence experiments, Surface Plasmon Resonance (SPR) and computational studies demonstrate that these complexes behave as selective probe for G-quadruplex structures.