Citation: Zhi Quan YONG, Xiao Ping XU, Ying Chun CHEN, Xu BAO, Ling Ling WENG, Hu ZHENG. Synthesis and Cytotoxic Activity of Novel Water-soluble Prodrugs of Combretastatin A-4[J]. Chinese Chemical Letters, ;2006, 17(1): 23-26. shu

Synthesis and Cytotoxic Activity of Novel Water-soluble Prodrugs of Combretastatin A-4

Department of Medicinal Chemistry, West China School of Pharmacy, Sichuan University, Chengdu 610041

Received Date: 18 May 2005

Fund Project: The project sponsored by SRF for ROCS, SEM. We are also grateful for the financial support from the grant of Sichuan University.

Novel water-soluble prodrugs of combretastatin A-4(5-8) were synthesized and evaluated for their in vitro cytotoxicity against lung carcinoma A549. Compound 5, bearing phosphoryl choline (PC) moiety, showed 90% inhibition at 32μg/mL concentration after 24 h. The findings showed the PC derivative would be a promising candidate for the development of new water-soluble prodrug of cytotoxic combretastatin A-4.
- Combretastatin A-4,
- cytotoxicity,
- phosphoryl choline,
- water-soluble,
- prodrug
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