Shaoxing University, School of Chemistry and Chemical Engineering, Zhejiang P.R China.
Expert Opin Ther Pat. 2011 Nov;21(11):1743-53. doi: 10.1517/13543776.2011.629190.
Norcantharidin (7-oxabicyclo [2.2.1] heptane-2,3-dicarboxylic anhydride) is the demethylated form of cantharidin. Norcantharidin not only has strong anticancer activity, but also eliminates most side-effects in the urinary system, does not cause myelosuppression and increases the number of white blood cells. With structural modification, norcantharidin analogues show potential anticancer activities.
A comprehensive patent review of norcantharidin analogues from 2006 to 2010 is presented. Protein phosphatase 1, 2A, 2B and 5 inhibitors are described. The review summarizes the new compounds and lays the foundation for seeking more effective anticancer compounds.
Although norcantharidin has improved activity and toxicity, the effects routinely do not satisfy the current clinical need. Exploring better analogues is vital for changing the current situation, but norcantharidin is a good lead compound.
去甲斑蝥素（7-氧杂双环[2.2.1]庚烷-2,3-二羧酸酐）是斑蝥素的脱甲基形式。去甲斑蝥素不仅具有很强的抗癌活性，而且还消除了泌尿系统中的大多数副作用，不会引起骨髓抑制并增加白细胞数量。通过结构修饰，去甲斑蝥素类似物显示出潜在的抗癌活性。
对 2006 年至 2010 年去甲斑蝥素类似物进行了全面的专利审查。描述了蛋白磷酸酶 1、2A、2B 和 5 抑制剂。综述总结了新的化合物，为寻找更有效的抗癌化合物奠定了基础。
虽然去甲斑蝥素的活性和毒性得到了改善，但效果通常不能满足当前的临床需求。探索更好的类似物对于改变现状至关重要，但去甲斑蝥素是一个很好的先导化合物。
