Overexpression of Human Epidermal Growth Factor Receptor (HER2) occurs in around 30% of breast cancers. In HER2 positive resistant breast cancers, three main isoforms are found: WT-HER2, the truncated p95HER2, and HER2Δ16. We focus more on the HER2Δ16, mainly because HER2Δ16 is found in resistant breast cancers and aggressive tumor growth. Of the many growth inhibitors tested in our laboratory, 5,8-dihydroxynaphtoquinones was found to be the most effective growth inhibitors of HER2Δ16 overexpressed MCF7 breast cancer cell lines. Currently, the objective is to synthesize new derivatives from our lead compound to improve the inhibition potency. Using a synthetic sequence that involved bromination, formylation, and Wittig reactions, a new derivative was formed from these multiple steps. A Witting product (1, 4, 5, 8-tetramethoxy-2-vinylnapthalene) was made and in the future we plan to create further derivatives and test them in bioassay trials.<br/>

Development of new novel therapeutics for refractive breast cancer

253rd National Meeting (2017)

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