In-vitro anticancer profile of recent ruthenium complexes against liver cancer

Ruthenium complexes are considered as the most favorable alternatives to traditional platinum-based cancer drugs owing to their acceptable toxicity level, selectivity, variant oxidation states and ability to treat platinum-resistant cancer cells. They have similar ligand exchange kinetics as platinum drugs but can be tailored according to our desire by ligands influence. In the current study, we illustrate the in-vitro anticancer profile of some ruthenium complexes (2016-2021) against human hepatocellular carcinoma (HepG2). The anticancer activity of ruthenium complexes is determined by comparing their IC50 values with one another and positive controls. Fortunately, some ruthenium complexes including 3, 4, 6, 14, 15, 20, 42, and 48 exhibit surpassed in-vitro anticancer profile than that of positive controls promising as potential candidates against liver cancer. We also explored the structure-activity relationship (SAR) which is a key factor in the rational designing and synthesis of new ruthenium drugs. It covers the factors affecting anticancer activity including lipophilicity, planarity, area and bulkiness, the steric influence of different ligands, and electronic effects induced by ligands, stability, aqueous solubility and bioavailability to the target sites. The data reported here will provide strong support in the plausible design and synthesis of ruthenium anticancer drugs in the upcoming days.

Automated summary

Ruthenium complexes are considered as promising alternatives to platinum-based cancer drugs due to their acceptable toxicity level, selectivity, variant oxidation states, and ability to treat platinum-resistant cancer cells. This study demonstrates the in-vitro anticancer activity of several ruthenium complexes against hepatocellular carcinoma, with some complexes showing superior activity compared to positive controls. The structure-activity relationship analysis provides insights for the design and synthesis of new ruthenium anticancer drugs.