DNA-Binding and Anticancer Activity of Pyrene-Imidazolium Derivatives

Anna Maria Pia Salvo, Michela Giuliano, Riccardo Bonsignore, Angelo Spinello, Michelangelo Gruttadauria, Francesco Giacalone, Antonietta Notaro, Alessio Terenzi, Giampaolo Barone, Alessio Terenzi, Anna Maria Pia Salvo, Bernhard K. Keppler, Antonietta Notaro, Angelo Spinello, Riccardo Bonsignore, Giampaolo Barone, Giuseppe Fiasconaro, Francesco Giacalone, Michelangelo Gruttadauria, Michela Giuliano

Research output: Contribution to journalArticlepeer-review

5 Citations (Scopus)


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.
Original languageEnglish
Pages (from-to)6755-6761
Number of pages7
Publication statusPublished - 2016

All Science Journal Classification (ASJC) codes

  • General Chemistry


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