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.

Terenzi, A., Ducani, C., Blanco, V., Zerzankova, L., Westendorf, A.F., Peinador, C., et al. (2012). DNA Binding Studies and Cytotoxicity of a Dinuclear PtII Diazapyrenium- Based Metallo-supramolecular Rectangular Box. CHEMISTRY-A EUROPEAN JOURNAL, 18, 10983-10990 [10.1002/chem.201201519].

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

TERENZI, Alessio;BARONE, Giampaolo;
2012-01-01

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*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.
2012
Settore CHIM/03 - Chimica Generale E Inorganica
Settore CHIM/08 - Chimica Farmaceutica
Settore CHIM/06 - Chimica Organica
Settore BIO/10 - Biochimica
Terenzi, A., Ducani, C., Blanco, V., Zerzankova, L., Westendorf, A.F., Peinador, C., et al. (2012). DNA Binding Studies and Cytotoxicity of a Dinuclear PtII Diazapyrenium- Based Metallo-supramolecular Rectangular Box. CHEMISTRY-A EUROPEAN JOURNAL, 18, 10983-10990 [10.1002/chem.201201519].
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/10447/64278
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