细胞毒性 N-(芴甲氧羰基)-二肽（Fmoc）：结构-活性关系和协同研究。
Cytotoxic N-(fluorenyl-9-methoxycarbonyl) (Fmoc)-dipeptides: structure-activity relationships and synergistic studies.
机构信息
Graduate Institute of Natural Products, Kaohsiung Medical University, Kaohsiung 807, Taiwan.
出版信息
Eur J Med Chem. 2010 Jun;45(6):2494-502. doi: 10.1016/j.ejmech.2010.02.035. Epub 2010 Mar 1.
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.
描述了一系列基于 Fmoc 的二肽的合成和细胞毒性评价。在所合成的 30 个化合物中，化合物 4a、8a、12a、2b、4b、10b、3c、4c 和 6c 对 HepG2、Hep3B、MCF-7、MDA-MB-231、A549 和 Ca9-22 人癌细胞系表现出较强的活性。最具活性的化合物（10a 和 10c）对 HepG2 和 Ca9-22 细胞系的敏感性相对较好，IC50 值分别为 1.0 和 0.4μM。此外，化合物 10c 对 Ca9-22 细胞系的活性比阳性对照阿霉素强 3 倍。此外，10c 对 MDA-MB-231 癌细胞系的阿霉素表现出协同作用，增加了其细胞毒性。因此，10c 可用作治疗开发的新先导化合物。
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