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

Časopis: CHEMISTRY-A EUROPEAN JOURNAL 18, 10983-10990
Autoři: Terenzi, A., Ducani, C., Blanco, V., Zerzankova, L., Westendorf, AF., Peinador, C., Quintela, JM., Bednarski, PJ., Barone, G., Hannon, MJ.
Rok: 2012


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 5x105?M-1, whereas the metallacycle 2 binds and bends the DNA with a binding constant of 7x106M-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 mu M and shows similar levels of efficacy, but a different spectrum of activity, to cisplatin.