目的:设计斑蝥素衍生物合成路线,寻找低毒有效的新型斑蝥素衍生物.方法:以呋喃和顺丁烯二酸酐为初始原料经多步合成斑蝥素衍生物,其结构经1H NMR和IR确证；并分别通过家兔眼刺激性实验方法和MTT法,以去甲斑蝥素(NCTD)为对照,考查衍生物的刺激性毒性和体外抗癌活性.结果:合成得到3种斑蝥素衍生物a,b和c,药理结果表明化合物a,b和c均对肿瘤细胞株有一定的抑制作用,且他们的刺激性毒性顺序为:a＞ NCTD＞ c＞b.结论:合成路线简易可行,得到的衍生物刺激性毒性很小,有进一步研究的价值.%objective: To design synthetic route of cantharidin derivatives and look for novel low toxic effective can-tharidin derivatives. methods: Cantharidin derivatives were synthesized through several steps using furan and maleic anhydride as the starting material, all compounds were confirmed by 1H NMR and IR. ; With norcanthadin (NCTD) as control sample, excitant toxicity was investigated by eye irritation of experimental methods and antitumor activity in vitro was investigated by MTT. results: Three cantharidin derivatives a、b and c was obtained; each derivative have certain inhibition on tumor cell line; excitant toxicity order was: a > NCTD > c > b. conclusion: The synthetic route was simple and feasible, the excitant toxicity of obtained derivatives was small and had the the value of further study.
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