Synthesis of Novel N-Heterocyclic Carbene-Ruthenium (II) Complexes, Precious Tools with Antibacterial, Anticancer and Antioxidant Properties

Ruthenium N-heterocyclic carbene (Ru-NHC) complexes show interesting physico-chemical properties as catalysts and potential in medicinal chemistry, exhibiting multiple biological activities, among them anticancer, antimicrobial, antioxidant, and anti-inflammatory. Herein, we designed and synthesized a new series of Ru-NHC complexes and evaluated their biological activities as anticancer, antibacterial, and antioxidant agents. Among the newly synthesized complexes, RANHC-V and RANHC-VI are the most active against triple-negative human breast cancer cell lines MDA-MB-231. These compounds were selective in vitro inhibitors of the human topoisomerase I activity and triggered cell death by apoptosis. Furthermore, the Ru-NHC complexes' antimicrobial activity was studied against Gram-positive and -negative bacteria, revealing that all the complexes possessed the best antibacterial activity against the Gram-positive Staphylococcus aureus, at a concentration of 25 mu g/mL. Finally, the antioxidant effect was assessed by DPPH and ABTS radicals scavenging assays, resulting in a higher ability for inhibiting the ABTS(center dot+), with respect to the well-known antioxidant Trolox. Thus, this work provides encouraging insights for further development of novel Ru-NHC complexes as potent chemotherapeutic agents endowed with multiple biological properties.

Automated summary

Ruthenium N-heterocyclic carbene (Ru-NHC) complexes were designed, synthesized, and evaluated for their biological activities. The complexes displayed significant anticancer activity against triple-negative human breast cancer cell lines MDA-MB-231. They also showed potent antibacterial activity against Gram-positive bacteria Staphylococcus aureus and strong antioxidant ability.