Small Molecular Leads Differentially Active Against HER2 Positive and Triple Negative Breast Cancer Cell Lines

(E-pub Ahead of Print)

Author(s): Adnan Badran, Atia-tul-Wahab, Sharmeen Fayyaz, Elias Baydoun, M. Iqbal Choudhary*.

Journal Name: Medicinal Chemistry

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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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(E-pub Ahead of Print)
DOI: 10.2174/1573406414666181106143912
Price: $95

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