Organometallic compounds have gained popularity as potent anti-cancer therapeutic prospects in recent years. The constant threat of drug-resistant cancer and the limited specificity of anti-cancer drugs, which necessitate the urgent development of novel anti-cancer agents, are the principal obstacles to controlling and eradicating cancer. Primarily ferrocene derivatives, considered a prime example of an organometallic compound, have remarkable structural and mechanistic diversity, inherent stability against air and temperature, low toxicity, inexpensive, reversible redox properties, ligand exchange, and catalytic properties, making them promising potential drugs for cancer prevention and treatment. Significant effort has been made to isolate and synthesize ferrocene derivatives with improved anti-cancer activity due to the prospective utilization of ferrocene in the treatment of cancer chemotherapy. In order to assist both academics and researchers interested in the development of novel and effective pharmaceuticals to address cancer therapy in this discipline, we have focused our efforts in this review article on providing a broad overview of the most recent research publications of ferrocenyl moieties with potential applications in cancer treatment (2015-present).