We have been exploring the antitumoral potential of the DNA cleaving activity mediated by copper compounds. Previously, we proposed that the cytotoxic action of some artificial dinuclear copper compounds was related to DNA cleavage by a hydrolytic mechanism. Four copper(II) complexes containing an antibiotic molecule (tetracycline, doxycycline, or 2-furoic acid hydrazide) and a heterocyclic nitrogen compound (1,10-phenanthroline or 2,2-bipyridine) as ligands cleave DNA and inhibit the growth of a chronic myelogenous leukemia cell line. The cytotoxic activity correlates well with the intracellular copper concentration and the number of Cu-DNA adducts formed inside cells. A substitution of doxycycline for tetracycline leads to an increase in the activity, while the substitution of 2,2-bipyridine for 1,10-phenanthroline renders the complex less active. The compounds cleave DNA molecule in mild conditions and in the absence of additional agents. UV-light exposure increases the cytotoxic activities of the compounds, which makes them potential agents for photodynamic therapy.

Correlation between antitumoral and DNA cleavage activities of some complexes of Cu(II)

243rd National Meeting (2012)

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