摘要
Aim To design and synthesize norcantharidin disodium phosphate derivatives. Methotis Diels-Alder reaction between furan and maleic anhydride afforded dehydronorcantharidin, and subsequent hydrogenation, phosphorylation, and basification gave compounds 1 and 2, separately. Resuits The structures of compounds were confirmed by IR, NMR and FAB-MS. The aqueous solubility of 1 and 2 were improved, compared with the parent compounds, and their activities were more potent than norcantharidin 4 against MGCS03 cell lines. Conclusion The phosphorylation of norcantharidin analogues is an effective way to increase the activity and solubility.
目的设计合成去甲斑蝥素的磷酸二钠盐。方法呋喃和顺丁烯二酸酐经过Diels-Alder制得去甲去氢斑蝥素,再通过一系列的加氢、磷酸化,碱化等反应,制得目标化合物1和2。结果成功合成了去甲斑蝥素磷酸二钠盐,其药理活性以及水溶性较母体化合物有很大提高。结论磷酸化是提高此类药物活性和水溶性的有效手段。
基金
NaturalScienceFoundationofGuangdongProvince(040022461)
ScienceandTechnologyProgramofGuangdongProvince(2003B31603)
