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报道一种新型蛋白磷酸酶抑制剂的高效合成方法及其结构表征。L-组氨酸和去甲斑蝥素在95%乙醇中回流,缩合生成L-组氨酸去甲斑蝥酰亚胺。该反应收率为97.0%,远远高于文献值。更重要的是,缩合产物保持了L-立体构型。利用IR,FAB-MS,~1H NMR,~(13)C NMR和2D NMR(~1H,~(13)C-COSY和HMBC)等对缩合产物进行了结构表征;此外,还首次报道了包括其旋光度在内的物理常数数据。初步的细胞毒性评价表明,与去甲斑蝥素相比,目标化合物在生长抑制活性试验中对一些人体癌细胞株显示了更好的抑制活性。氨基酸去甲斑蝥酰亚胺的设计与合成为(去甲)斑蝥素衍生物结构改造提供了新思路。
Reported a novel high-performance protein phosphatase synthesis method and its structural characterization. L-histidine and norcantharidin were refluxed in 95% ethanol to condense L-histidine nor-cantharidimide. The reaction yield was 97.0%, much higher than the literature value. More importantly, the condensation product maintains the L-stere configuration. The condensation products were characterized by IR, FAB-MS, 1H NMR, 13C NMR and 2D NMR (~ 1H, ~ (13) C-COZY and HMBC). In addition, Its optical rotation, including the physical constant data. Preliminary cytotoxicity evaluations showed that the target compounds showed better inhibitory activity against some human cancer cell lines in the growth inhibitory activity assay than norcantharidin. The design and synthesis of amino acid norcantharidin provide a new idea for structural modification of (nor-nor-cantharidin) derivatives.