Abstract

Photoirradiation of O-hydroxylcyclohexyletheramine-doxorubicin (dox) when bound to DNA exhibits high DNA cleavage efficiency and selectivity, leading to GG steps cleavage. Coupling ultraviolet absorption with viscosity measurement, the mode of dox–DNA complex is groove-binding. The three-dimensional structure from X-ray crystallography reveals that dox bound to DNA base pairs to groove reversal along with its antenna (hydroxylcyclohexylether-amine) in the major groove. We also provide a direct evidence of supporting a model that transfers electrons from base to dox and holes migrate within DNA.

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