Small molecular leads differentially active against HER2 positive and triple negative breast cancer cell lines
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Bentham Science Publishers
Abstract
Background: Breast cancer is the most prevalent cancer type in women globally. It is characterized by distinct subtypes depending on different gene expression patterns. 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. Methods: The current study evaluates and compares the anti-breast cancer effect of commercially available compounds against HER2 overexpressing BT-474, and triple 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 (4), a steroidal lactone glycoside, showed the most potent activity with IC50 values of 0.63 ± 0.56, and 0.69 ± 0.59 µM against BT-474 and MDA-MB-231, respectively, whereas 4-[4-(Trifluoromethyl)-phenoxy] phenol (3) a phenol derivative, and Reserpine (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 cancers in vitro. © 2019 Bentham Science Publishers.
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Anti-cancer, Breast cancer, Convallatoxin, Estrogen receptors, Heterocyclic compounds, Human epidermal growth factor receptor-2 (her2), Antineoplastic agents, Breast neoplasms, Cell proliferation, Cell survival, Dose-response relationship, drug, Drug screening assays, antitumor, Female, Fibroblasts, Humans, Molecular structure, Protein kinase inhibitors, Receptor, erbb-2, Small molecule libraries, Structure-activity relationship, Triple negative breast neoplasms, Tumor cells, cultured, 4 [4 (trifluoromethyl)phenoxy]phenol, 8 quinolinol, Antineoplastic agent, Cloxiquine, Doxorubicin, Phenol derivative, Reserpine, Unclassified drug, Zerumbone, Epidermal growth factor receptor 2, Erbb2 protein, human, Protein kinase inhibitor, Antineoplastic activity, Article, Breast cancer cell line, Bt-474 cell line, Cancer inhibition, Controlled study, Drug cytotoxicity, Drug selectivity, Human, Human cell, Human epidermal growth factor receptor 2 positive breast cancer, Ic50, In vitro study, Mda-mb-231 cell line, Priority journal, Triple negative breast cancer, Breast tumor, Chemical structure, Chemistry, Dose response, Drug effect, Drug screening, Fibroblast, Metabolism, Molecular library, Pathology, Pharmacology, Structure activity relation, Synthesis, Tumor cell culture