本文概述了三大经典代表斑蝥类化合物的来源和物化性质，综述了其合成策略和基本合成路线。随后着重综述了斑蝥素和去甲斑蝥素及其衍生物的基本概况，及其近年来在抗肿瘤方面的研究进展，特别是其与抗癌机理密切相关的特异性结合酶，丝/苏氨酸蛋白磷酸酯酶（PP）中PP1、PP2A 和PP2B的抑制活性和选择性的构效关系。总结了斑蝥类新型生物活性小分子的设计和发展方向。

This study was aimed to summarize main-bone structure of cantharidin-based small molecules and facts about three typical candidates including its origin, physical-chemical properties and general synthetic approaches.Basic chemical and pharmacological information as well as development of anti-cancer activities, which were related to cantharidin, norcantharidin and their analogues were reviewed, especially the relationship between the structures and their inhibitory activity and selectivity of serine-threonine protein phosphatases PP1, PP2A and PP2B in cancer treatment. The designs and developments of new biological cantharidin-based small molecules were also reviewed.

重庆市科委科技平台与基地建设（科研院所创新能力建设）项目（cstc2012pt-kyys10004）：中药新产品开发研究能力提升建设，负责人：唐安明；重庆市科委科技平台与基地建设（科研院所创新能力建设）项目（cstc2012pt-kyys10001）：重庆市GLP 中心能力提升建设，负责人：杨大坚。