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斑蝥素(Ⅰ)是我国传统中药斑蝥抗肿瘤作用的有效成分。其双去甲基类似物去甲斑蝥素(Ⅱ)有与Ⅰ类似的抗癌活性,对早、中期肝癌疗效较好、且毒性较Ⅰ低,并有升高白细胞的作用,已应用于临床。我们设计和合成了一系列去甲斑蝥素的类似物和衍生物,以期寻找高效低毒的抗肿瘤化合物。前文报道了去甲斑蝥素氨基酸衍生物的合成与抗癌活性,本文报道去氧脱氢类似物(见图1)的合成与活性初筛结果。
Cantharidin (Ⅰ) is an effective component of the antitumor effect of traditional Chinese medicine Cantharidin. Its dual-demethyl catechin, Norcantharidin (Ⅱ), has anti-cancer activity similar to that of Ⅰ and has good curative effect on early-stage and middle-stage liver cancer with low toxicity and increased white blood cell function, which has been applied to clinical . We have designed and synthesized a series of analogues and derivatives of norcantharidin with a view to finding highly effective and low toxicity antitumor compounds. The synthesis and anticancer activity of norcantharidinyl amino acid derivatives have been reported previously. The results of the synthesis and activity screening of deoxy-desorbed analogues (see Figure 1) were reported.