Antibacterial and Cytotoxic Activity of Ruthenium-p-cymene Complexes with 2-Methylquinolin-8-ol Derivatives

Nain-Perez, AmalynGothenburg University,Göteborgs universitet,Institutionen för kemi och molekylärbiologi,Department of Chemistry and Molecular Biology (author)

Eight 5-aryl-2-methylquinolin-8-ol ligands (2-9) were prepared by a cross-coupling Suzuki reaction from precursors brominated at position 5 (10), and positions 5 and 7 (11). These ligands were converted into new ruthenium(II)-p-cymene complexes (12-22) (51-94 %). The cytotoxic and antimicrobial activities of all compounds were investigated. Ligands showed higher cytotoxicity (EC50=3.1-4.8 mu M) than ruthenium complexes (EC50=5.2-7.8 mu M) against human melanoma cancer cells (A375). The most potent compound 7 has been shown to act via apoptosis. Some compounds were more potent as anticancer than cisplatin. Several ruthenium complexes selectively inhibited S. typhimurium and S. aureus (IC50=4.64-146.15 and 9.37-125.95 mu g/mL, respectively), while most ligands were potent against C. albicans. Molecular docking studies with a protein from S. aureus suggest four key amino acids interactions, in agreement with the inhibitory potential against this bacterium.

Barbosa, L. C. A. (author)
Araujo, M. H. (author)
Martins, J. P. A. (author)
Takahashi, J. A. (author)
Oliveira, G. (author)
Diniz, R. (author)
Heller, L. (author)
Hoenke, S. (author)
Csuk, R. (author)
Göteborgs universitetInstitutionen för kemi och molekylärbiologi (creator_code:org_t)

By the author/editor: Nain-Perez, Amal ...; Barbosa, L. C. A ...; Araujo, M. H.; Martins, J. P. A ...; Takahashi, J. A.; Oliveira, G.; show more...; Diniz, R.; Heller, L.; Hoenke, S.; Csuk, R.; show less...

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