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

• 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.

Subject headings

MEDICIN OCH HÄLSOVETENSKAP  -- Klinisk medicin (hsv//swe)

MEDICAL AND HEALTH SCIENCES  -- Clinical Medicine (hsv//eng)

Keyword

antibacterial

anticancer

cytotoxicity

quinoline derivatives

ruthenium

Chemistry

Publication and Content Type

ref (subject category)

art (subject category)