Progress Towards a Norcantharidin-based Scaffold for Inhibition of the Protein Phosphatase 5C (PP5C) Enzyme

Madison R. Tuttle, Edward A. Salter, Andrzej Wierzbicki, Richard E. Honkanen, Larry Yet

Abstract


Recent studies have shown that the overexpression of PP5C is associated with invasive ductal carcinoma of the breast, cancer cell proliferation and resistance to apoptosis. Screening and computational efforts revealed a series of potentially selective and potent small molecule chemical probes containing a 5-(3-amino)-propoxymethyl-(7-oxabicyclo[2.2.1]heptane) scaffold for PP5C. In attempt to further characterize the biological and pathological roles of PP5C in the antitumor activity of breast cancer, a multi-step synthesis scheme was devised to construct the scaffold. This work details the unsuccessful experimental procedures developed for the construction of the 5-(3-amino)-propoxymethyl-(7-oxabicyclo[2.2.1]heptane) scaffold, as well as a discussion on other possible synthesis methods.


Keywords


Norcantharidin; PP5C; breast cancer; Finkelstein; Williamson ether

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