Background: Breast cancer is the most prevalent cancer type in women globally. It is
characterized by distinct subtypes depending on different gene expression pattern. Oncogene
HER2 is expressed on the surface of cell, and is responsible for cell growth regulation. Increase in
HER2 receptor protein due to gene amplification, results in aggressive growth, and high metastasis
in cancer cells.
Method: The current study evaluates and compares the anti-breast cancer effect of commercially
available compounds against HER2 overexpressing BT-474, and estrogen and HER2 negative
MDA-MB-231 breast cancer cell lines.
Results: Preliminary in vitro cell viability assays on these cell lines identified 6 lead molecules active
against breast cancer. Convallatoxin, a steroidal lactone glycoside, showed the most potent activity
with IC50 values of 0.63 ± 0.56, and 0.69 ± 0.08 μM against BT-474 and MDA-MB-231, respectively,
whereas compounds 3 a phenol derivative, and compound 5 an indole alkaloid selectively
inhibited the growth of BT-474, and MDA-MB-231 breast cancer cells, respectively.
Conclusion: These results exhibited the potential of small molecules in the treatment of HER2
amplified and triple negative breast cancer in vitro.
Keywords: Anti-cancer, Breast cancer, Human epidermal growth factor receptor-2 (HER2), Estrogen receptors, Heterocyclic compounds, Convallatoxin.
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