Improved synthesis and structure identification of L-histidine norcantharimide , a potent PP2A inhibitor was reported. Condensation between norcantharidin and L-histidine in 95% EtOH at reflux temperature affords L-hi...Improved synthesis and structure identification of L-histidine norcantharimide , a potent PP2A inhibitor was reported. Condensation between norcantharidin and L-histidine in 95% EtOH at reflux temperature affords L-histidine norcantharimide in 97.0f% yield which is much higher compared with literature, and more importantly, the configuration is retained. The chemical structure of the compound was re-elucidated through IR, FAB-MS, ^1H NMR, ^13C NMR and 2D NMR （^1H, ^13C-COSY and HMBC）, the fundamental physical data, including optical data being also firstly reported. Preliminary cytotoxicity evaluation showed that the target compound was probably more potent than norcantharidin against a panel of human cancer cell lines. Design and synthesis of amino acid （nor） cantharirnides would provide a convenient and rational structure modification of （nor） cantharidin and open new avenues to explore new promising candidates.展开更多
基金Science and Technology Program of Guangdong Province(Grant No.2006B35604002)Guangzhou City(Grant No.2007JI-C0261).
文摘Improved synthesis and structure identification of L-histidine norcantharimide , a potent PP2A inhibitor was reported. Condensation between norcantharidin and L-histidine in 95% EtOH at reflux temperature affords L-histidine norcantharimide in 97.0f% yield which is much higher compared with literature, and more importantly, the configuration is retained. The chemical structure of the compound was re-elucidated through IR, FAB-MS, ^1H NMR, ^13C NMR and 2D NMR （^1H, ^13C-COSY and HMBC）, the fundamental physical data, including optical data being also firstly reported. Preliminary cytotoxicity evaluation showed that the target compound was probably more potent than norcantharidin against a panel of human cancer cell lines. Design and synthesis of amino acid （nor） cantharirnides would provide a convenient and rational structure modification of （nor） cantharidin and open new avenues to explore new promising candidates.
