5-Ene-2-arylaminothiazol-4(5H)-ones Induce Apoptosis in Breast Cancer Cells

As breast cancer remains a significant challenge for the current medical field, molecules with a 4-thiazolidinone scaffold can become promising candidates for addressing the increasing threat of cancer. This study aims to develop and evaluate the novel 4-thiazolidinone derivatives with anticancer potential. New compounds were synthesized through two different pathways, one as a two-step process and the other as a one-pot method. The second approach fits the requirements of cost-effective methodologies and allows for the reduction of synthetic steps, reagents, and reaction time. The obtained data from in vitro research showed a potent cytotoxic activity of the novel structures in micromolar concentrations against MCF-7 breast cancer cells. Further investigations into their anticancer activity revealed that the tested compounds induced apoptosis through intrinsic and extrinsic pathways, which was evidenced by their capability to reduce the mitochondrial membrane potential and induce the activation of caspases 7, 8, 9, and 10. A more detailed analysis uncovered that one of the novel compounds can affect the expression of key apoptotic proteins, tumor protein P53 (p53), cytochrome C, and Bax in treated cells. Additionally, these compounds displayed an enhanced generation of reactive oxygen species (ROS) in MCF-7 cells, which suggests that ROS-mediated mechanisms can take part in the anticancer potential of the synthesized compounds.

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Publication Details

Journal
Cells
Published
2025-06-07
DOI
https://doi.org/10.3390/cells14120861
Citations
1
Primary Topic
Synthesis and biological activity
Type
article
Field-Weighted Citation Impact
0.94

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article

5-Ene-2-arylaminothiazol-4(5H)-ones Induce Apoptosis in Breast Cancer Cells

Serhii Holota, Rostyslav Dudchak, Anna Bielawska, Ivan Sydorenko et al.
1 citations
Cells
Synthesis and biological activity
0.94
article

5-Ene-2-arylaminothiazol-4(5H)-ones Induce Apoptosis in Breast Cancer Cells

Serhii Holota, Rostyslav Dudchak, Anna Bielawska, Ivan Sydorenko, Agnieszka Gornowicz, Robert Czarnomysy, Krzysztof Bielawski, Roman Lesyk, Magdalena Podolak, Olexandr Karpenko
article en
1 citations

Abstract

As breast cancer remains a significant challenge for the current medical field, molecules with a 4-thiazolidinone scaffold can become promising candidates for addressing the increasing threat of cancer. This study aims to develop and evaluate the novel 4-thiazolidinone derivatives with anticancer potential. New compounds were synthesized through two different pathways, one as a two-step process and the other as a one-pot method. The second approach fits the requirements of cost-effective methodologies and allows for the reduction of synthetic steps, reagents, and reaction time. The obtained data from in vitro research showed a potent cytotoxic activity of the novel structures in micromolar concentrations against MCF-7 breast cancer cells. Further investigations into their anticancer activity revealed that the tested compounds induced apoptosis through intrinsic and extrinsic pathways, which was evidenced by their capability to reduce the mitochondrial membrane potential and induce the activation of caspases 7, 8, 9, and 10. A more detailed analysis uncovered that one of the novel compounds can affect the expression of key apoptotic proteins, tumor protein P53 (p53), cytochrome C, and Bax in treated cells. Additionally, these compounds displayed an enhanced generation of reactive oxygen species (ROS) in MCF-7 cells, which suggests that ROS-mediated mechanisms can take part in the anticancer potential of the synthesized compounds.

CellsVol. 14(12)
Medical University of Białystok (PL), Taras Shevchenko National University of Kyiv (UA), Danylo Halytsky Lviv National Medical University (UA), University of Information Technology and Management in Rzeszow (PL), Enamine (Ukraine) (UA)
National Research Foundation of Ukraine, National Research Foundation
Good health and well-being
Openalex Percentile: Top 25%
Synthesis and biological activity
0.94
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