Tunable Anticancer Activity of Furoylthiourea‐Based Ru^II–Arene Complexes and Their Mechanism of Action

Abstract

Fourteen new RuII–arene (p‐cymene/benzene) complexes (C1–C14) have been synthesized by varying the N‐terminal substituent in the furoylthiourea ligand and satisfactorily characterized by using analytical and spectroscopic techniques. Electrostatic potential maps predicted that the electronic effect of the substituents was mostly localized, with some influence seen on the labile chloride ligands. The structure–activity relationships of the Ru–p‐cymene and Ru–benzene complexes showed opposite trends. All the complexes were found to be highly toxic towards IMR‐32 cancer cells, with C5 (Ru–p‐cymene complex containing C6H2(CH3)3 as N‐terminal substituent) and C13 (Ru–benzene complex containing C6H4(CF3) as N‐terminal substituent) showing the highest activity among each set of complexes, and hence they were chosen for further study. These complexes showed different behavior in aqueous solutions, and were also found to catalytically oxidize glutathione. They also promoted cell death by apoptosis and cell cycle arrest. Furthermore, the complexes showed good binding ability with the receptors Pim‐1 kinase and vascular endothelial growth factor receptor 2, commonly overexpressed in cancer cells.

Multi-Biofunctional Properties of Phytofabricated Selenium Nanoparticles From Carica papaya Fruit Extract: Antioxidant, Antimicrobial, Antimycotoxin, Anticancer, and Biocompatibility

“…The micro-morphological observation study concluded that SeNPs have selectively influenced the cellular damage in cancer cells. Thus, SeNPs were found to be biocompatible toward normal cells ( Swaminathan et al, 2019 , 2021 ).…”

“…The cytotoxic effects of SeNPs on both normal and cancerous cell populations were measured using the MTT assay, which was determined by the cellular proliferation rate and cell viability (Swaminathan et al, 2019(Swaminathan et al, , 2021Kota et al, 2021). The methodology is provided in the Supplementary Data [(10) Cell viability and micro-morphology assessment].…”

Impact of Biphenyl Benzhydrazone-Incorporated Arene Ru(II) Complexes on Cytotoxicity and the Cancer Cell Death Mechanism

“…Rhodamine 123, a green fluorescent cationic dye, has been used to measure the mitochondrial membrane potential. It stains the viable cells of mitochondria in the membrane potential-dependent fashion . The concentration of the dye has been noticed to investigate the mitochondrial functions of the treated and untreated cancer cells.…”

Impact of denticity of chromone/chromene thiosemicarbazones in the ruthenium(II)‐DMSO complexes on their cytotoxicity against breast cancer cells

“…The basis set used for the analyses was LANL2DZ with B3LYP functional. [27,28] The optimized structures and calculated bond lengths are shown in Figure 2 and Table 1, respectively. The bond lengths were in accordance with those reported for similar Ru(II)-DMSO complexes.…”