Title:Development of Anticancer Agents from Plant-Derived Sesquiterpene Lactones
VOLUME: 23 ISSUE: 23
Author(s):Yulin Ren, Jianhua Yu and A. Douglas Kinghorn
Affiliation:Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, Columbus, OH 43210, United States.
Keywords:Artemisinin, Dimers of artemisinin, Dimethylaminoparthenolide, Parthenolide, Potential anticancer
agents, Sesquiterpene lactones, Thapsigargin.
Abstract:Sesquiterpene lactones are of considerable interest due to their potent
bioactivities, including cancer cell cytotoxicity and antineoplastic efficacy in in
vivo studies. Among these compounds, artesunate, dimethylaminoparthenolide,
and L12ADT peptide prodrug, a derivative of thapsigargin, are being evaluated in
the current cancer clinical or preclinical trials. Based on the structures of several
antitumor sesquiterpene lactones, a number of analogues showing greater potency
have been either isolated as natural products or partially synthesized, and some
potential anticancer agents that have emerged from this group of lead compounds
have been investigated extensively. The present review focuses on artemisinin,
parthenolide, thapsigargin, and their naturally occurring or synthetic analogues
showing potential anticancer activity. This provides an overview of the advances
in the development of these types of sesquiterpene lactones as potential anticancer
agents, including their structural characterization, synthesis and synthetic
modification, and antitumor potential, with the mechanism of action and
structure-activity relationships also discussed. It is hoped that this will be helpful
in stimulating the further interest in developing sesquiterpene lactones and their
derivatives as new anticancer agents.
