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Design and Synthesis of Disodium Phosphate Derivatives of Norcantharidin

ZHOU Yue, CAI Yu-chen, ZHANG Xue-jing, WANG Zhi-xin, XIAN Li-jian, ZOU Yong*   

  1. 1.Guangzhou Institute of Chemistry, Chinese Academy of Sciences, Guangzhou 510650, China;
    2.Cancer Center of Zhongshan University, Guangzhou 510060, China
  • Received:2005-12-20 Revised:2006-02-10 Online:2006-03-15 Published:2006-03-15
  • Contact: ZOU Yong*

Abstract: Aim To design and synthesize norcantharidin disodium phosphate derivatives. Methods Diels-Alder reaction between furan and maleic anhydride afforded dehydronorcantharidin, and subsequent hydrogenation, phosphorylation, and basification gave compounds 1 and 2, separately. Results 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 MGC803 cell lines. Conclusion The phosphorylation of norcantharidin analogues is an effective way to increase the activity and solubility.

Key words: norcantharidin, norcantharidin, disodium phosphate, disodium phosphate, design, design, synthesis, synthesis

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