The article discusses the development and potential of organometallic compounds as anticancer agents, focusing on their structural diversity, unique properties, and mechanisms of action. Organometallics, defined as metal complexes with direct metal–carbon bonds, offer advantages such as structural variety, stereochemistry, and kinetic stability, making them promising candidates for medicinal chemistry. The article highlights various classes of organometallic compounds, including metallocenes, carbene, and CO ligands, and their applications in anticancer therapy. Ferrocene, a well-known metallocene, has been studied for its antiproliferative effects, with derivatives like ferroquine showing potential as antimalarial drugs. The article also discusses the redox activity of ferrocene and its derivatives, which can lead to the formation of reactive intermediates that interact with DNA or proteins. In the context of ruthenium-based compounds, the article examines the mechanism of action of RAPTA derivatives, which differ from cisplatin in their target and mode of action. These compounds are found to bind to proteins such as cathepsin B and thioredoxin reductase, rather than DNA. The article also explores the use of organometallic complexes in targeting specific enzymes and proteins, such as glutathione transferase, and their potential in cancer therapy. For osmium-based compounds, the article notes their potential as antitumor agents, despite their lower solubility and inertness compared to ruthenium. The study of osmium complexes, such as those with picolinate ligands, shows promising anticancer activity. The article also discusses the role of triosmium clusters in inhibiting telomerase, an enzyme crucial for cancer progression. Finally, the article covers the investigation of iridium and rhodium-based organometallic compounds, which have shown potential in binding to DNA through intercalation of polypyridyl ligands. These compounds are being studied for their antitumor properties and their ability to interact with cellular targets. Overall, the article emphasizes the importance of organometallic compounds in the development of new anticancer drugs, highlighting their unique properties and potential for targeted therapy.The article discusses the development and potential of organometallic compounds as anticancer agents, focusing on their structural diversity, unique properties, and mechanisms of action. Organometallics, defined as metal complexes with direct metal–carbon bonds, offer advantages such as structural variety, stereochemistry, and kinetic stability, making them promising candidates for medicinal chemistry. The article highlights various classes of organometallic compounds, including metallocenes, carbene, and CO ligands, and their applications in anticancer therapy. Ferrocene, a well-known metallocene, has been studied for its antiproliferative effects, with derivatives like ferroquine showing potential as antimalarial drugs. The article also discusses the redox activity of ferrocene and its derivatives, which can lead to the formation of reactive intermediates that interact with DNA or proteins. In the context of ruthenium-based compounds, the article examines the mechanism of action of RAPTA derivatives, which differ from cisplatin in their target and mode of action. These compounds are found to bind to proteins such as cathepsin B and thioredoxin reductase, rather than DNA. The article also explores the use of organometallic complexes in targeting specific enzymes and proteins, such as glutathione transferase, and their potential in cancer therapy. For osmium-based compounds, the article notes their potential as antitumor agents, despite their lower solubility and inertness compared to ruthenium. The study of osmium complexes, such as those with picolinate ligands, shows promising anticancer activity. The article also discusses the role of triosmium clusters in inhibiting telomerase, an enzyme crucial for cancer progression. Finally, the article covers the investigation of iridium and rhodium-based organometallic compounds, which have shown potential in binding to DNA through intercalation of polypyridyl ligands. These compounds are being studied for their antitumor properties and their ability to interact with cellular targets. Overall, the article emphasizes the importance of organometallic compounds in the development of new anticancer drugs, highlighting their unique properties and potential for targeted therapy.