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.

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Publication Details

Journal
Scientia Pharmaceutica
Published
2026-09-29
DOI
https://doi.org/10.3390/scipharm94040087
Primary Topic
Synthesis and biological activity
Type
article
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article

5-((5-Nitrofuran-2-yl)allylidene)-2-thioxo-4-thiazolidinones Target Microtubules in Breast Cancer Cells

Małgorzata Borzym‐Κluczyk, Olga Klaudia Szewczyk-Roszczenko, Rostyslav Dudchak, Anna Bielawska et al.
Scientia Pharmaceutica
Synthesis and biological activity
article

5-((5-Nitrofuran-2-yl)allylidene)-2-thioxo-4-thiazolidinones Target Microtubules in Breast Cancer Cells

Małgorzata Borzym‐Κluczyk, Olga Klaudia Szewczyk-Roszczenko, Rostyslav Dudchak, Anna Bielawska, Agnieszka Gornowicz, Krzysztof Bielawski, Roman Lesyk, Yegor S Vassetzky, Magdalena Podolak
article en

Abstract

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.

Scientia PharmaceuticaVol. 94(4)
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)
Good health and well-being
Openalex Percentile: Top 22%
Synthesis and biological activity
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5-((5-Nitrofuran-2-yl)allylidene)-2-thioxo-4-thiazolidinones Target Microtubules in Breast Cancer Cells — Małgorzata Borzym‐Κluczyk, Olga Klaudia Szewczyk-Roszczenko, et al. · Scientia Pharmaceutica (2026) | TGRS Research Map | TGRS