Divergent Synthesis and Identification of the Cellular Targets of Deoxyelephantopins
The sesquiterpene lactone Deoxyelephantopin is the most active ingredient in extracts of Elephantopus scaber.1 Biological investigations have demonstrated cytotoxicity against several human cancer cell lines, and cytotoxicity superior to that of Paclitaxel in breast cancer models.2 Moreover, it suppresses proteasome activity,3 inhibits the NF-κB pathway4 and is a partial PPARγ agonist.5
A divergent synthesis of Deoxyelephantopin analogues and their biological evaluation will be presented, including the identified pharmacophores, novel potential drug targets and the binding mode with PPARγ.6
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