Cancer is one of the deadliest diseases worldwide. Chemotherapy remains one of the frequently applied treatment modalities in the clinics. However, as the currently applied agents are associated with severe side effects, scientists are searching for novel chemotherapeutic drugs. Within the last decades, Cu(II) polypyridine complexes have received increasing attention as potential anticancer drug candidates. Herein, the biological activity of terminally functionalised mono- and bis-coordinated Cu(II)-2,2':6',2 ''-terpyridine complexes have been investigated. The bis-coordinated compounds were found to have a cytotoxic effect in the nanomolar range in human adenocarcinomic alveolar basal epithelial cells. Promisingly, the complexes were equally active in the corresponding cisplatin resistant cell line, indicating that they could potentially be useful for the treatment of drug resistant tumours.