<p>Ruthenium Complexes as Anticancer Agents: A Brief History and Perspectives</p>

Abstract

Platinum (Pt)-based anticancer drugs such as cisplatin have been used to treat various cancers. However, they have some limitations including poor selectivity and toxicity towards normal cells and increasing chemoresistance. Therefore, there is a need for novel metallo-anticancers, which has not been met for decades. Since the initial introduction of ruthenium (Ru) polypyridyl complex, a number of attempts at structural evolution have been conducted to improve efficacy. Among them, half-sandwich Ru-arene complexes have been the most prominent as an anticancer platform. Such complexes have clearly shown superior anticancer profiles such as increased selectivity toward cancer cells and ameliorating toxicity against normal cells compared to existing Pt-based anticancers. Currently, several Ru complexes are under human clinical trials. For improvement in selectivity and toxicity associated with chemotherapy, Ru complexes as photodynamic therapy (PDT), and photoactivated chemotherapy (PACT), which can selectively activate prodrug moieties in a specific region, have also been investigated. With all these studies on these interesting entities, new metalloanticancer drugs to at least partially replace existing Pt-based anticancers are anticipated. This review covers a brief description of Ru-based anticancer complexes and perspectives.

A Novel Ruthenium(II) Complex With Lapachol Induces G2/M Phase Arrest Through Aurora-B Kinase Down-Regulation and ROS-Mediated Apoptosis in Human Prostate Adenocarcinoma Cells

“…Ruthenium complexes have been extensively reported as potent cytotoxic and anti-metastatic agents in different cancer cells ( 52 , 53 ); however, the incorporation of bioactive ligands enhances the biological activity of the metal complex formed. Ruthenium(II) complexes designed in the present study were tested against several cancer cells, presenting important cytotoxic activity.…”

Synthesis and Structural Characterization of Half-Sandwich Arene–Ruthenium(II) Complexes with Bis(imidazol-1-yl)methane, Imidazole and Benzimidazole

“…Ruthenium complexes are of interest as catalysts, and they have also emerged as promising nonplatinum antitumor or antimetastatic agents [1][2][3][4][5][6]. A great number of ruthenium complexes with potential antitumor activity have been developed to date.…”

Preclinical Pharmacokinetics and Biodistribution of Anticancer Dinuclear Palladium(II)-Spermine Complex (Pd2Spm) in Mice

“…Even though from the thermodynamic point of view, a Pt-ligand bond in conventional platinum(II) coordination compounds presents somewhat lower thermodynamic durability (≤100 kJ/mol) than single and double covalent bonds between C–C, C–N or C–O (250–500 kJ/mol), the ligand substitution is rather slow, yielding reasonably stable molecules with desired in vivo pharmacokinetic and pharmacodynamic properties [ 10 , 11 ]. In addition to numerous platinum compounds developed in recent decades [ 9 ], complexes containing other transition metals have also been investigated, including palladium(II) [ 12 ], gold(I), gold(II), tin(IV) [ 13 ], ruthenium(II), ruthenium(III) [ 14 ] and copper(II)-based compounds [ 15 ]. Palladium(II) complexes have received particular interest as potential Pt(II) analogs thanks to the similarities in structure and coordination chemistry between these two metal ions [ 12 , 16 ].…”