TY - JOUR
T1 - Cytotoxic N-(fluorenyl-9-methoxycarbonyl) (Fmoc)-dipeptides
T2 - Structure-activity relationships and synergistic studies
AU - Yen, Chiao Ting
AU - Wu, Chin Chung
AU - Lee, Jin Ching
AU - Chen, Shu Li
AU - Morris-Natschke, Susan L.
AU - Hsieh, Pei Wen
AU - Wu, Yang Chang
PY - 2010/6
Y1 - 2010/6
N2 - 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.
AB - 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.
KW - Ca9-22
KW - Cytotoxicity
KW - Fmoc-based dipeptide
KW - HepG2
KW - Human cancer cell line
UR - http://www.scopus.com/inward/record.url?scp=77950859907&partnerID=8YFLogxK
U2 - 10.1016/j.ejmech.2010.02.035
DO - 10.1016/j.ejmech.2010.02.035
M3 - 文章
C2 - 20334960
AN - SCOPUS:77950859907
SN - 0223-5234
VL - 45
SP - 2494
EP - 2502
JO - European Journal of Medicinal Chemistry
JF - European Journal of Medicinal Chemistry
IS - 6
ER -