DNA Binding Studies and Cytotoxicity of a Dinuclear Pt(II) Diazapyrenium-Based Metallo-supramolecular Rectangular Box |
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Authors: | Alessio Terenzi Cosimo Ducani Víctor Blanco Lenka Zerzankova Aron F Westendorf Carlos Peinador José M Quintela Patrick J Bednarski Giampaolo Barone Michael J Hannon |
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Affiliation: | School of Chemistry, University of Birmingham, Edgbaston, Birmingham B15 2TT (UK); Dip. di Scienze e Tecnologie Molecolari e Biomolecolari (STEMBIO), Università di Palermo, Sezione di Chimica Farmaceutica e Biologica, Via Archirafi, 32-90123 Palermo (Italy). |
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Abstract: | The interaction with native DNA of a 2,7-diazapyrenium-based ligand 1 and its Pt(II) 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 5×10(5) M(-1) , whereas the metallacycle 2 binds and bends the DNA with a binding constant of 7×10(6) 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 IC(50) values ranging between 3.1 and 19.2?μM and shows similar levels of efficacy, but a different spectrum of activity, to cisplatin. |
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