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DNA Binding Studies and Cytotoxicity of a Dinuclear PtII Diazapyrenium- Based Metallo-supramolecular Rectangular Box

  • Autori: Terenzi, A.; Ducani, C.; Blanco, V.; Zerzankova, L.; Westendorf, A.; Peinador, C.; Quintela, J.; Bednarski, P.; Barone, G.; Hannon, M.
  • Anno di pubblicazione: 2012
  • Tipologia: Articolo in rivista (Articolo in rivista)
  • Parole Chiave: cytotoxicity; metallodrugs; noncovalent DNA binding; PtII rectangular box; supramolecular chemistry
  • OA Link:


The interaction with native DNA of a 2,7-diazapyrenium-based ligand 1 and its PtII rectangular metallacycle 2 is explored through circular and linear dichroism and fluorescence spectroscopies. The metal-free ligand 1 binds through intercalation, with a binding constant of approximately 5*105m-1, whereas the metallacycle 2 binds and bends the DNA with a binding constant of 7*106m-1. PCR assays show that metallo-supramolecular box 2 interferes with DNA transactions in vitro whereas the intercalator 1 does not. The metallacycle is active against four human cancer cell lines, with IC50 values ranging between 3.1 and 19.2 mm and shows similar levels of efficacy, but a different spectrum of activity, to cisplatin.