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Dna‐binding and anticancer activity of pyrene‐imidazolium derivatives

Bonsignore, Riccardo, Notaro, Antonietta, Salvo, Anna Maria Pia, Spinello, Angelo, Fiasconaro, Giuseppe, Terenzi, Alessio, Giacalone, Francesco, Keppler, Bernhard K., Giuliano, Michela, Gruttadauria, Michelangelo and Barone, Giampaolo 2016. Dna‐binding and anticancer activity of pyrene‐imidazolium derivatives. ChemistrySelect 1 (21) , pp. 6755-6761. 10.1002/slct.201601502

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DNA‐binding investigations showed that two different derivatives endowed with pyrene and imidazolium moieties, 1 and 2, strongly bind both double‐stranded DNA and telomeric sequences in G‐quadruplex (G4) conformation. The values of the DNA‐binding constants indicate that 1 and 2 show preferential affinity for G4‐DNA, of about one and two orders of magnitude, respectively. Moreover, 1 and 2 inhibit short and long‐term proliferation of breast cancer cell lines in a time‐ and dose‐dependent fashion. Remarkably, senescence assays indicate that telomeric G4‐DNA is a possible biotarget for the cytotoxic activity of 2. Molecular dynamics simulations suggest that the stronger binding of 2 with G4‐DNA and the related senescence induction, are a consequence of additional edge‐to‐face interactions with a base in the TTA loop.

Item Type: Article
Date Type: Publication
Status: Published
Schools: Chemistry
ISSN: 2365-6549
Date of Acceptance: 2 December 2016
Last Modified: 16 Oct 2020 01:45

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