Introduction: The fused aromatic system of terpyridines makes them good, innocent ligands for various metals. The resulting complexes have been extensively studied for both their biological activity and physico-chemical properties. However, although free ligands also have an interesting biological activity, their share in recent research is considerably limited.
Areas covered: This review covers the literature on the anticancer activity of terpyridines with special attention being paid to their use as free ligands. Whenever possible, the mechanism of action has been discussed, thereby providing evidence of the substantial differences between sole ligands or less stable complexes and those that have heavier elements.
Expert opinion: The existing literature indicates that there is a specific attitude for investigating terpyridines and their transition metal complexes. While the latter have been well explored and recognized in the scientific community, the free terpyridines are considered to be useful solely due to their complexing ability. At the same time, terpyridines could have similar or even higher anticancer potency than their complexes. Moreover, a mechanistic analysis of the stability and intracellular activity would provide information that would be useful for designing new drugs.
Keywords: Terpyridine; anticancer; chelators; complexes; metal-based drugs; reactive oxygen species.