The bioorganometallic chemistry of ferrocene has been gaining significance in recent years. This review presents ferrocene-triazole conjugates displaying significant biological properties. The conjugates have been synthesized via azide-alkyne cycloaddition reactions. The data are summarized according to the type of activity (anticancer, antibacterial and/or antifungal, antiprotozoal, and other effects). The results of studies concerning the understanding of the role of the ferrocene core in their biological activity are highlighted. While generally the mode of action of these organometallic species remains unclear, the importance of redox properties of ferrocene has been postulated in several cases.