Cytotoxic N-(fluorenyl-9-methoxycarbonyl) (Fmoc)-dipeptides: Structure-activity relationships and synergistic studies

Chiao Ting Yen, Chin Chung Wu, Jin Ching Lee, Shu Li Chen, Susan L. Morris-Natschke, Pei Wen Hsieh*, Yang Chang Wu

*Corresponding author for this work

Research output: Contribution to journalJournal Article peer-review

18 Scopus citations

Abstract

The synthesis and cytotoxic evaluation of a series of Fmoc-based dipeptides are described. Among the thirty compounds, 4a, 8a, 12a, 2b, 4b, 10b, 3c, 4c and 6c showed potent activity against HepG2, Hep3B, MCF-7, MDA-MB-231, A549 and Ca9-22 human cancer cell lines. The most active compounds (10a and 10c) showed relatively good sensitivity toward HepG2 and Ca9-22 cell lines with IC50 values of 1.0 and 0.4 μM, respectively. Additionally, compound 10c was threefold more potent than doxorubicin, the positive control, against the Ca9-22 cell line. Furthermore, 10c showed a synergistic effect and increased the cytotoxicity of doxorubicin against the MDA-MB-231 cancer cell line. Therefore, 10c could be used as a new lead compound for therapeutic development.

Original languageEnglish
Pages (from-to)2494-2502
Number of pages9
JournalEuropean Journal of Medicinal Chemistry
Volume45
Issue number6
DOIs
StatePublished - 06 2010

Keywords

  • Ca9-22
  • Cytotoxicity
  • Fmoc-based dipeptide
  • HepG2
  • Human cancer cell line

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