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Cantharidin as an Antitumor Agent: A Retrospective Review

[ Vol. 20 , Issue. 2 ]


L.P. Deng, J. Dong, H. Cai and W. Wang   Pages 159 - 166 ( 8 )


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.


Cantharidin, norcantharidin, antitumor, structure-activity relationship, medicinal chemistry, antitumor agent, norcantharimide, enormous efforts, mechanistic studies, intriguing bioactivities


Department of Pharmacology, Chemistry and Chemical Engineering Institute, Shaoxing University, Shaoxing, Zhejiang 312000, China.

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