ArticlePloS one2025
Thionated levofloxacin derivative: Potential repurposing for cancer treatment and synergism with doxorubicin on doxorubicin-resistant lung cancer cells.
Article in PloS one, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.
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Who cites it
4 citing papers in PubMed.
- Systems Biology and Experimental Validation Enable Discovery of MMP9-Centered Networks, Anticancer Activity, and Pharmacodynamic Signature in Non-Small Cell Lung Cancer.International journal of molecular sciences · 2026Article
- Biodesulfurization and activation of a thionated levofloxacin derivative: antimicrobial evaluation and LC-MS-based metabolic profiling.Naunyn-Schmiedeberg's archives of pharmacology · 2026Article
- Antioxidant Properties of Novel Lipophilic Fluoroquinolone Compounds Against Oxidative Stress Induced by Acetaminophen and Carbon Tetrachloride in Male Wistar Rats.Biomolecules · 2026Article
- Thiourea Derivatives for the Potential Treatment of Lung Cancer via the Inhibition of EGFR and Efflux Pumps: Synthesis,Anti-cancer agents in medicinal chemistry · 2026Article
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Authors and funding
9 authors.
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Abstract
objectivesFluoroquinolones, such as levofloxacin (LVX), are extended-spectrum drugs used for the treatment of bacterial infections. Several fluoroquinolone derivatives have shown promising antibacterial and anticancer activities. Our group has earlier synthesized and investigated thionated LVX analogs, compounds 2 and 3, on A549 (non-small cell lung cancer) cell line and showed promising anticancer activity. The mechanism of cytotoxicity may be, in part, via aldehyde dehydrogenase enzyme inhibition and antioxidation. In this study, compounds 2 and 3 were evaluated on prostate (PC-3), breast (MCF7), colorectal (Caco-2), and small cell lung cancer (H69 and H69AR) cell lines.
methodsThe anticancer activity was measured using resazurin colorimetric method. Combination treatments with doxorubicin (DOX) were also employed and combination index (CI) value were calculated.
resultsCompound 3 possessed higher anticancer activity compared to compound 2 on the tested cancer cell lines. Compound 3 had the highest activity on PC-3 cells with IC50 value of 3.58 µM. DOX was also tested for comparison and had IC50 value of less than 0.5 µM in all tested cell lines except for H69AR (DOX-resistant form of H69), which was 4.62 µM. Combination treatment with DOX resulted in significant reduction of cell viability in PC-3, H69, and H69AR cells, with those on H69 and H69AR cells resulted in additive (CI = 1.0) and synergistic effects (CI = 0.6), respectively.
conclusionsCompound 3, a thionated LVX derivative, showed a promising anticancer activity, prompting its potential repurposing for cancer treatment as well as combination treatment with DOX on DOX-resistant cancer cells.
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