Organometallic chemistry has allowed the design and emergence of a new class of metal-based bioactive molecules and a variety of drugs already used or being tested against cancer. In this field, cisplatin is well-known and widely used clinically. However, recent contributions are focusing on the functionalization of clinically validated purely organic drugs with complexes derivatized by a metallocene group. This approach has been shown to exalt the anti-cancer properties of the organic moiety, and has been successfully used to design ferrocifens. These complexes involve a ferrocenyl group covalently grafted onto the tamoxifen skeleton, the current gold standard for endocrine breast cancer therapy. Based on the same strategy, several original ruthenocene- and osmocene-tamoxifen derivatives have been recently synthesized and were also successfully tested against breast and other cancer cells.

This communication will detail how the development of such potent metallodrugs was directly bearing on the accurate mechanistic understanding of their electron transfer activation provided by the synergistic combination of molecular electrochemistry and biological approaches.