Dna‐binding and anticancer activity of pyrene‐imidazolium derivatives

Bonsignore, Riccardo ORCID: https://orcid.org/0000-0003-2699-4384, 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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Abstract

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:	07 Nov 2022 09:19
URI:	https://orca.cardiff.ac.uk/id/eprint/128682

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