Cancer, a highly heterogeneous disease at intra/inter patient levels, remains a serious health
problem contributing to significant morbidity and mortality worldwide. Despite great progress in
clinical treatment, the concern impeding the success of conventional cancer chemotherapy is descending
efficacy of anticancer agents due to the development of drug resistance especially multiple drug
resistance (MDR). Ferrocene derivatives have a different mode of action to the platinum anticancer
drugs, and the ferrocene-phenol hybridferrocifen exhibits potentialactivity againstdrug-resistant cancers.
Currently, ferrocifen is in preclinical trial, demonstrating that ferrocene derivatives are useful
scaffolds for the development of novel anticancer candidates which are active against drug-resistant
cancers. In the present review, the current scenario of ferrocene derivatives including ferrocenemetal
complexes, hybrids and other derivatives with antiproliferative potential against drug-resistant cancer
cell lines is summarized for further rational design.