Synthesis of pharmaceutically relevant terpene derivatives for use as topoisomerase inhibitors

Abstract

Topoisomerase inhibitors play an important role in the fight against cancer. The focus of this research is to create a suite of pharmaceutically relevant terpene derivatives that can then be evaluated for usefulness in inhibiting topoisomerase. Multiple aldehydes have been chosen to be evaluated, all containing 19F. The targets of this work are terpenoids based on the diterpene carvone. The target molecules have synthetic handles that allow expansion to a known family of topoisomerase inhibiting diterpenes, the trachylobane family. While the inclusion of the 19F label here allows for the analysis of the protein interactions that these terpenoids participate in. The scope of this synthesis and the novel molecules produced were evaluated for reproducibility and usefulness in the inhibition of topoisomerase.