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As cancer remains the second leading cause of death in the United States, investigations into new cancer treatments are at the forefront of research efforts. The chemotherapeutic cisplatin has remained one of the most effective anticancer drugs; however, it has numerous toxic side effects and its overuse has resulted in cisplatin resistant tumors. Chemotherapeutics with differing mechanisms of action may help to combat resistance and may be less toxic to healthy cells. The work presented here is focused on the synthesis and characterization of a series of schiff-base containing copper compounds and assessment of these complexes for their anticancer properties. Preliminary investigations into the biological activity of these new complexes included DNA cleavage studies and cancer cell proliferation assays. In particular, complex-induced supercoiled DNA cleavage was observed in vitro, as demonstrated by an increase in both single and double nicked DNA with increasing complex concentration. The toxicity of the complexes was also tested against HeLa, PC-3, and MCF7 cancer cell lines and IC50 values were determined and compared to cisplatin. Importantly, the complexes showed a concentration dependent inhibition of cell growth across all cell lines tested with IC50 values in the micromolar range. Ongoing studies are focused on further understanding the mechanism of action of these complexes. Investigations into the cytotoxicity of the complexes to noncancerous cells are also underway, and will provide additional evidence to assess the potential application of these complexes as new chemotherapeutics.
Stein et al. (Fri,) studied this question.