Abstract

A new dinuclear copper(II) complex, [Cu(DPA)OH]2⋅2ClO4(Cu2-DPA2, DPA = di(pyridin-2-yl)amine), was synthesized and structurally characterized. The complex crystallized in a triclinic P-1 space group, taking on a slightly distorted tetragonal geometry. Both Cu(II) in Cu2-DPA2 are bridged by two hydroxyl groups with a distance of 2.938 A. The whole molecule is nearly co-planar with the exception of the bridging hydroxyl groups. Complex Cu2-DPA2 can cleave efficiently supercoiled pBR322 DNA into its nicked and linearized forms at micromolar concentrations in the presence of ascorbate near physiological conditions. The presence of standard radical scavengers does not have any apparent effect on the cleavage efficiency, suggesting that Cu(II) bound oxygen intermediates rather than freely diffusible hydroxyl radicals may act as the active species in the DNA scission. Comparison of the cleavage reactivity of Cu2-DPA2 with that of mononuclear analogue Cu-DPA and trinuclear Cu3-L demonstrates that the synergistic effect between Cu(II) centers in Cu2-DPA2 is crucial for the DNA cleavage.

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