HER2 overexpression in breast cancer tumors predicts lower overall survival. Because of the aggressive nature of HER2 tumors and the association with metastatic disease, the HER2 receptor holds great promise as a therapeutic target in metastatic breast cancer. We are developing small molecule inhibitors that bind to the ATP binding site of the tyrosine kinase domain in order to inhibit tyrosine autophosphorylation. This process controls biological pathways that mediate the cell growth. In normal cells this process is highly controlled. We are targeting the modification of the side chain of the hydroxymethyl group of 2-hydroxy methyl-5, 8-dimethoxy-1, 4-naphthaquinone. These compounds should inhibit the tyrosine kinase cascade of reactions thereby suppressing the overexpression of HER2 shutting down the tumor growth. In this poster, we will present the inhibition and synthesis of a series of 2-hydroxy methyl-5, 8-dimethoxy-1, 4-naphthaquinone analogs.AcknowledgementThis work was supported by Department of Defence Breast Cancer Research Program, Partnership Training Award (W81XWH11-1-0105) and Western Kentucky University.

Functionalization and modification of 2-hydroxymethyl-5, 8-dimethoxy-1, 4-naphthaquinone as HER2 inhibitors

246th National Meeting (2013)

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