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Antibacterial and C...
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Nain-Perez, AmalynGothenburg University,Göteborgs universitet,Institutionen för kemi och molekylärbiologi,Department of Chemistry and Molecular Biology
(author)
Antibacterial and Cytotoxic Activity of Ruthenium-p-cymene Complexes with 2-Methylquinolin-8-ol Derivatives
- Article/chapterEnglish2021
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LIBRIS-ID:oai:gup.ub.gu.se/306587
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https://gup.ub.gu.se/publication/306587URI
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https://doi.org/10.1002/slct.202100733DOI
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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.
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Barbosa, L. C. A.
(author)
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Araujo, M. H.
(author)
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Martins, J. P. A.
(author)
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Takahashi, J. A.
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Oliveira, G.
(author)
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Diniz, R.
(author)
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Heller, L.
(author)
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Hoenke, S.
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Csuk, R.
(author)
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Göteborgs universitetInstitutionen för kemi och molekylärbiologi
(creator_code:org_t)
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In:Chemistryselect: Wiley6:12, s. 2942-29502365-6549
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Nain-Perez, Amal ...
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Barbosa, L. C. A ...
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Araujo, M. H.
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Martins, J. P. A ...
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Takahashi, J. A.
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Oliveira, G.
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Diniz, R.
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Heller, L.
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Hoenke, S.
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Csuk, R.
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- MEDICAL AND HEALTH SCIENCES
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Chemistryselect
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University of Gothenburg