5-((5-Nitrofuran-2-yl)allylidene)-2-thioxo-4-thiazolidinones Target Microtubules in Breast Cancer Cells
4-Thiazolidinone derivatives, a group of compounds with a broad spectrum of activity and anticancer properties, are used in medicine as anti-inflammatory, antiviral, antibacterial, antidiabetic, and blood pressure-lowering drugs; some of them are now in phase II and III clinical trials as anticancer drugs. Here, we evaluated the anticancer potential of 4-thiazolidinones (2b, 12b, 14b) targeting tubulin and metastasis-related pathways in breast cancer models. Molecular docking revealed that compound 14b exhibited the strongest binding affinity to the paclitaxel-binding site of β-tubulin, outperforming 2b and 12b, though slightly weaker than Taxol. Biological assays confirmed significant tubulin inhibition, with 14b reducing β-tubulin levels up to eight-fold in MCF-7 cells and two-fold in MDA-MB-231 cells. All compounds promoted tubulin polymerization, showing paclitaxel-like activity, with comparable the maximum velocity (Vmax) values. Cell cycle analysis demonstrated G2/M arrest in MCF-7 cells and S-phase accumulation in MDA-MB-231 cells. Overall, compound 14b demonstrated the most promising multitarget anticancer activity in vitro.
Authors
- Małgorzata Borzym‐Κluczyk (ORCID: https://orcid.org/0000-0001-7692-4179)
- Olga Klaudia Szewczyk-Roszczenko (ORCID: https://orcid.org/0000-0002-3719-6583)
- Rostyslav Dudchak
- Anna Bielawska (ORCID: https://orcid.org/0000-0001-9164-8440)
- Agnieszka Gornowicz (ORCID: https://orcid.org/0000-0002-0945-7870)
- Krzysztof Bielawski (ORCID: https://orcid.org/0000-0003-3187-4205)
- Roman Lesyk (ORCID: https://orcid.org/0000-0002-3322-0080)
- Yegor S Vassetzky (ORCID: https://orcid.org/0000-0003-3101-7043)
- Magdalena Podolak
Institutions
- Centre National de la Recherche Scientifique (FR)
- Medical University of Białystok (PL)
- Danylo Halytsky Lviv National Medical University (UA)
- Institut Gustave Roussy (FR)
- University of Information Technology and Management in Rzeszow (PL)
Publication Details
- Journal
- Scientia Pharmaceutica
- Published
- 2026-09-29
- DOI
- https://doi.org/10.3390/scipharm94040087
- Primary Topic
- Synthesis and biological activity
- Type
- article
- Field-Weighted Citation Impact
- 0.00