2. Academic Validation
  3. Synthesis and cytotoxic activity of novel derivatives of 4'-demethylepipodophyllotoxin

Synthesis and cytotoxic activity of novel derivatives of 4'-demethylepipodophyllotoxin

  • Bioorg Med Chem Lett. 2004 Oct 18;14(20):5063-6. doi: 10.1016/j.bmcl.2004.07.094.
Shi-Wu Chen 1,  Xuan Tian,  Yong-Qiang Tu
Affiliations

Affiliation

  • 1 State Key Laboratory of Applied Organic Chemistry and Department of Chemistry, Lanzhou University, Lanzhou 730000, PR China.
PMID: 15380199 DOI: 10.1016/j.bmcl.2004.07.094
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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