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  • Title: Synthesis and cytotoxic activity of novel derivatives of 4'-demethylepipodophyllotoxin.
    Author: Chen SW, Tian X, Tu YQ.
    Journal: Bioorg Med Chem Lett; 2004 Oct 18; 14(20):5063-6. PubMed ID: 15380199.
    Abstract:
    Nine novel 4beta-N-substituted-5-FU-4'-demethylepipodophyllotoxin derivatives were synthesized and evaluated as potential antitumor agents. All of the target compounds showed more significant cytotoxic activity against HL-60 and A-549 in vitro than VP-16 and 5-FU. Among them, 4beta-N-substituted-phenylalanine 5-Fu pentyl ester-4'-demethylepipodophyllotoxin (9 g) was found to exhibit most potent cytotoxic activity against HL-60 and A-549 cell (IC50 is 0.04 and <0.01 microM, respectively).
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