Department of Pharmacology, Chemistry and Chemical Engineering Institute, Shaoxing University, Shaoxing, Zhejiang 312000, China.
Curr Med Chem. 2013;20(2):159-66. doi: 10.2174/092986713804806711.
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.
这篇综述总结了近年来在中药斑蝥素的药物化学方面所取得的进展，斑蝥素是一种有效的抗肿瘤药物。在斑蝥素的基础上合成了数千种类似物，其中一部分具有优异的性质，特别是去甲斑蝥素和去甲斑蝥酰胺。尽管已经付出了巨大的努力，但这些引人入胜的生物活性、机制、适应症及其相互作用仍然没有明确的定义。这篇综述提供了我们最新的认识，包括斑蝥素类似物的治疗用途、机制、构效关系（SAR）和有趣的性质。通过对斑蝥素类似物进行设计，并结合机制研究，为将新型抗肿瘤药物转化为临床应用奠定了基础。
