A New 2-Benzofuran-Linked Chalcone–Tamoxifen Combination for Targeting ER+ Breast Cancer

3rd International Conference on Chemo and BioInformatics, Kragujevac, September 25-26. 2025. (pp. 616-619) 

 

AUTOR(I) / AUTHOR(S): İpek Aydın, Sibel Cinar-Asa, Aysen Sagnak, Demet Coskun, Ferda Ari

 

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DOI:  10.46793/ICCBIKG25.616A

SAŽETAK / ABSTRACT:

Breast cancer is the most common malignancy among women worldwide. Despite the widespread use of various chemotherapy agents, the development of more effective and targeted treatment strategies is of critical importance. Tamoxifen, an estrogen receptor inhibitor, is widely used in the treatment of breast cancer; however, its resistance development and limiting effect create significant problems. Chalcone derivatives naturally found in plants are an important source of inspiration to enrich the repertoire of chemotherapeutics. Natural or synthetic derivatives of chalcones are being investigated in detail for their anticancer properties. In this study, it was aimed to evaluate the anticancer activity of a new treatment approach consisting of the combination of 2-benzofuran-linked chalcone complex and tamoxifen in MCF-7 breast cancer cells. The effects of 2-benzofuran-linked chalcone complex, tamoxifen and combination therapy on cell viability were determined by the SRB method. The determination of the death mode (apoptosis/necrosis) in cells was analyzed by the Annexin-V/Hoechst/Propidium Iodide triple staining method. In addition, colony formation abilities of the combination were tested.The results showed that the combination of 2-benzofuran-linked chalcone complex with tamoxifen increased cytotoxic activity and induced apoptosis in breast cancer cells in a dose- and time- dependent manner. It was also found that the colony formation capacity of the combination was inhibited. These results suggest that the combination of 2-benzofuran-linked chalcone complex and tamoxifen may be a promising and effective strategy in the treatment of breast cancer.

KLJUČNE REČI / KEYWORDS:

Chalcone Derivatives, Tamoxifen, Breast Cancer, Cytotoxicity

PROJEKAT / ACKNOWLEDGEMENT:

This work was supported by Scientific Research Projects (BAP) with project number FYL-2024-1706. We would like to thank the Bursa Uludag Molecular Cancer Research Laboratory (BUMKAL) for their valuable support and contributions throughout this study.

LITERATURA / REFERENCES:

  • Yao, J., Deng, K., Huang, J., Zeng, R., & Zuo, J. (2020). Progress in the Understanding of the Mechanism of Tamoxifen Resistance in Breast Cancer. Frontiers in Pharmacology, 11.
  • Ali, S., Rasool, M., Chaoudhry, H., N Pushparaj, P., Jha, P., Hafiz, A., Mahfooz, M., Abdus Sami, G., Azhar Kamal, M., Bashir, S., Ali, A., & Sarwar Jamal, M. (2016). Molecular mechanisms and mode of tamoxifen resistance in breast cancer. Bioinformation, 12, 135–139.
  • Dorssers, C. J., van der Flier, S., Brinkman, A., van Agthoven, T., Veldscholte, J., Berns, E. J. J., Klijn, J. G. M., Beex, L. V. A. M., & Foekens, J. A. (2001). Tamoxifen Resistance in Breast Cancer. Drugs, 61(12), 1721–1733.
  • Lai, W., Chen, J., Gao, X., Jin, X., Chen, G., & Ye, L. (2023). Design and Synthesis of Novel Chalcone Derivatives: Anti-Breast Cancer Activity Evaluation and Docking Study. International Journal of Molecular Sciences, 24(21), 15549.
  • Farhat, J., Alzyoud, L., Alwahsh, M., & Al-Omari, B. (2022). Structure–Activity Relationship of Benzofuran Derivatives with Potential Anticancer Activity. Cancers, 14(9), 2196.
  • Franken, N. A. P., Rodermond, H. M., Stap, J., Haveman, J., & van Bree, C. (2006a). Clonogenic assay of cells in vitro. Nature Protocols, 1, 2315–2319.