Title:Cantharidin as an Antitumor Agent: A Retrospective Review
VOLUME: 20 ISSUE: 2
Author(s):L.P. Deng, J. Dong, H. Cai and W. Wang
Affiliation:Department of Pharmacology, Chemistry and Chemical Engineering Institute, Shaoxing University, Shaoxing, Zhejiang 312000, China.
Keywords:Cantharidin, norcantharidin, antitumor, structure-activity relationship, medicinal chemistry, antitumor agent, norcantharimide, enormous efforts, mechanistic studies, intriguing bioactivities
Abstract:This review summarizes the progress that has been made recently in the medicinal chemistry of cantharidin, a potent antitumor
agent from traditional Chinese medicine. Thousands of analogs have been synthesized on the basis of cantharidin, a part of which shows
excellent properties, in particular, norcantharidin and norcantharimide. Despite the enormous efforts made, the intriguing bioactivities,
mechanism, indications, and their interplay are still ill-defined. This review provides our up-to-date understanding in connection with the
therapeutic use, mechanism, structure-activity relationship (SAR) and interesting properties of cantharidin analogs. Considerable development
in the design of cantharidin analogs, in combination with mechanistic studies, has laid a foundation for transforming novel antitumor
drugs into the clinic.
