Recent advances on the structural modification of parthenolide and its derivatives as anticancer agents

Parthenolide (PTL) is a sesquiterpene lactone derived from medicinal plant feverfew (Tanacetum parthenium). Recent studies have demonstrated that it has multiple pharmacological activities, especially in the treatment of various hematological and solid cancers. The superior anticancer activity of PTL suggests that it has the potential to be a first-line drug. However, due to the limited physical and chemical properties, as well as bioavailability, structural modification strategies are strongly recommended to improve the anticancer activity. This review describes representative PTL derivatives obtained by different modification strategies, which are reported to exert antiproliferative activities superior to the parent compound PTL. Furthermore, we also summarize their basic mechanisms on cancer-related signaling pathways, so as to explain the potential and characteristics of PTL and its derivatives in cancer therapy.

Automated summary

Parthenolide (PTL), derived from feverfew, has shown significant anticancer activity and has the potential to be a first-line drug. Structural modification strategies are recommended to enhance its anticancer activity. This review focuses on representative PTL derivatives and their mechanisms in cancer therapy.