2. Academic Validation
  3. Cytotoxic N-(fluorenyl-9-methoxycarbonyl) (Fmoc)-dipeptides: structure-activity relationships and synergistic studies

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

  • Eur J Med Chem. 2010 Jun;45(6):2494-502. doi: 10.1016/j.ejmech.2010.02.035.
Chiao-Ting Yen 1,  Chin-Chung Wu,  Jin-Ching Lee,  Shu-Li Chen,  Susan L Morris-Natschke,  Pei-Wen Hsieh,  Yang-Chang Wu
Affiliations

Affiliation

  • 1 Graduate Institute of Natural Products, Kaohsiung Medical University, Kaohsiung 807, Taiwan.
PMID: 20334960 DOI: 10.1016/j.ejmech.2010.02.035
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 microM, 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.

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