Porphyrins and metalloporphyrins are investigated extensively as potential anticancer drugs. They work as DNA binding agents as well as photosensitizers in photodynamic therapy. Conjugation of the macrocycle with organometallic complexes is a powerful tool to implement the water soly. of the adducts and to provide distinct cytotoxic properties. Herein, six fourfold-​sym. cationic porphyrin-​ruthenium(II) conjugates (P1-​P6) are considered, which differ from one another by the substituents on the RuII fragments, the linkage of the metal fragments to the porphyrin, and the total pos. charge. Their interaction with DNA sequences arranged in different conformations is investigated. The data suggest that the tested conjugates discriminate poorly between different DNA structures. Indeed, unfolded DNA works efficiently as a template for the cationic conjugates. Nevertheless, they are extremely efficient in cleaving the macromol. upon irradn., regardless of its structural arrangement.

DNA Targeting by Cationic Porphyrin-​Ruthenium(II) Conjugates

SPAGNUL, CINZIA;MION, GIULIANA;GIANFERRARA, TERESA;
2015

Abstract

Porphyrins and metalloporphyrins are investigated extensively as potential anticancer drugs. They work as DNA binding agents as well as photosensitizers in photodynamic therapy. Conjugation of the macrocycle with organometallic complexes is a powerful tool to implement the water soly. of the adducts and to provide distinct cytotoxic properties. Herein, six fourfold-​sym. cationic porphyrin-​ruthenium(II) conjugates (P1-​P6) are considered, which differ from one another by the substituents on the RuII fragments, the linkage of the metal fragments to the porphyrin, and the total pos. charge. Their interaction with DNA sequences arranged in different conformations is investigated. The data suggest that the tested conjugates discriminate poorly between different DNA structures. Indeed, unfolded DNA works efficiently as a template for the cationic conjugates. Nevertheless, they are extremely efficient in cleaving the macromol. upon irradn., regardless of its structural arrangement.
http://onlinelibrary.wiley.com/journal/10.1002/(ISSN)2192-6506/issues
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/11368/2833693
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