Cancer is considered as the biggest medicinal challenge worldwide. During a typical treatment, the tumorous tissue is removed in a surgical procedure and the patient further treated by chemotherapy. One of the most frequently applied drugs are platinum complexes. Despite their clinical success, these compounds are associated with severe side effects and low therapeutic efficiency. To overcome these limitations, herein, the synthesis and biological evaluation of Cu(II) terpyridine complexes as chemotherapeutic drug candidates is suggested. The compounds were found to be highly cytotoxic in the nanomolar range against various cancer cell lines. Mechanistic insights revealed that the compounds primarily accumulated in the cytoplasm and generated reactive oxygen species in this organelle, triggering cell death by apoptosis. Based on their high therapeutic effect, these metal complexes could serve as a starting point for further drug development.