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- Title
Tunable Anticancer Activity of Furoylthiourea‐Based Ru<sup>II</sup>–Arene Complexes and Their Mechanism of Action.
- Authors
Swaminathan, Srividya; Haribabu, Jebiti; Kalagatur, Naveen Kumar; Nikhil, Maroli; Balakrishnan, Nithya; Bhuvanesh, Nattamai S. P.; Kadirvelu, Krishna; Kolandaivel, Ponmalai; Karvembu, Ramasamy
- 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.
- Subjects
VASCULAR endothelial growth factor receptors; RUTHENIUM compounds; STRUCTURE-activity relationships; ELECTRIC potential; CANCER cells; POLAR effects (Chemistry)
- Publication
Chemistry - A European Journal, 2021, Vol 27, Issue 26, p7418
- ISSN
0947-6539
- Publication type
Academic Journal
- DOI
10.1002/chem.202004954