Parthenolide (PTL) is a plant-derived natural product from feverfew and a well-established active component of many natural medicines. Previous studies have demonstrated that PTL selectively targets the cancer stem cell population in acute myeloid leukemia (AML) without destroying normal hematopoietic stem cells. The selectivity for targeting cancer stem cells versus normal stem cells by a small molecule has generated excitement in the drug discovery community. Notably, cancer stem cells are highly resistant to chemotherapeutic drugs and treatment regimens that allow cancer stem cells to survive therapy may ultimately result in disease relapse. Our laboratory at the University of Minnesota has synthesized PTL pulldown probes (such as 1  ) to elucidate the mechanism of AML CSC toxicity by PTL. In addition, we prepared a number of novel PTL analogues (such as 2  ) and studied their activities with in vitro and in vivo models of AML. Our progress in both areas will be presented.

Synthesis and evaluation of parthenolide analogs: Chemical probes and therapeutic agents

244th National Meeting (2012)

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