The American Cancer Society estimates 250,000 new cases of breast cancer will be diagnosed in the United States this year, and just over 40,000 of those cases are expected to result in death. Although the primary tumors that remain in the breast are typically removable by surgery, the metastasis of the cancerous cells to vital organs often leads to mortality. Inhibiting the proteins that drive the metastasis of tumors is crucial to the prevention of lethal cancer progression. Inflammatory cytokines are a class of proteins that have been shown to increase levels of metastatic breast cancer due to their roles in cell detachment, migration, and invasion. This research project aims to synthesize a variety of small molecule inhibitors (SMIs) that interrupt the pathways leading to these events. Two families of SMIs are being prepared. The first, based on a bis-thiazole, is prepared by subjecting bromoacetoacetates to a Hantzsch thiazole synthesis, followed by a Perkin reaction using derivatized cinnamaldehydes. The second family, based on substituted furans, is prepared via a Suzuki reaction between dibrominated furfural and a variety of aryl boronic acids. The preparation of these inhibitors and preliminary biological assays will be reported. The described studies could lead to the development of novel therapeutics targeted against metastatic breast cancer.

Structure-based drug design of novel therapeutics targeting metastatic breast cancer

253rd National Meeting (2017)

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