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Current Medicinal Chemistry


ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

Cantharidin as an Antitumor Agent: A Retrospective Review

Author(s): L.P. Deng, J. Dong, H. Cai and W. Wang

Volume 20 , Issue 2 , 2013

Page: [159 - 166] Pages: 8

DOI: 10.2174/0929867311320020001

Price: $65


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.

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

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