The biological activity of two fluorescent Zn(II)-salophen derivatives has been evaluated. In vitro studies (AFM, emission and UV-vis titration with ethidium bromide and cell growth inhibition) show different mechanisms of interaction with DNA. It has been observed that these compounds enter the cells. Comet assays (with cultured fibroblast cells) have revealed that cellular uptake occurs without damaging the DNA strands. Preliminary studies carried out with living cells have shown IC50 values in a millimolar range, indicative of a non-cytotoxic behaviour. This fact could be understood by confocal microscopy co-localization studies with living cell internalization that have shown that, in fact, the compounds seem to enter the cells but not the nucleus under in vivo conditions.