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- Title
DNA Binding Studies and Cytotoxicity of a Dinuclear Pt<sup>II</sup> Diazapyrenium-Based Metallo-supramolecular Rectangular Box.
- Authors
Terenzi, Alessio; Ducani, Cosimo; Blanco, Víctor; Zerzankova, Lenka; Westendorf, Aron F.; Peinador, Carlos; Quintela, José M.; Bednarski, Patrick J.; Barone, Giampaolo; Hannon, Michael J.
- Abstract
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 5×105 M−1, whereas the metallacycle 2 binds and bends the DNA with a binding constant of 7×106 M−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 μ M and shows similar levels of efficacy, but a different spectrum of activity, to cisplatin.
- Publication
Chemistry - A European Journal, 2012, Vol 18, Issue 35, p10983
- ISSN
0947-6539
- Publication type
Article
- DOI
10.1002/chem.201201519