Aim To design and synthesize norcantharidin disodium phosphate derivatives. Methotis Diels-Alder reaction between furan and maleic anhydride afforded dehydronorcantharidin, and subsequent hydrogenation, phosphorylatio...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.展开更多
文摘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.