TY - JOUR
T1 - Design, synthesis, biological evaluation and molecular modeling studies of 1-aryl-6-(3,4,5-trimethoxyphenyl)-3(Z)-hexen-1,5-diynes as a new class of potent antitumor agents
AU - Lo, Yu Hsiang
AU - Lin, Ying Ting
AU - Liu, Yu Peng
AU - Duh, Tsai Hui
AU - Lu, Pei Jung
AU - Wu, Ming Jung
N1 - Funding Information:
We would like to thank the National Science Council of the Republic of China for the financial support.
PY - 2013/4
Y1 - 2013/4
N2 - A series of novel enediyne-containing molecules, 1-aryl-6-(3,4,5- trimethoxyphenyl)-3(Z)-hexen-1,5-diynes, were synthesized and displayed significant IC50 values of 10-7 to 10-6 M against various cancer cell lines. Of these compounds, 1-(2-pyridinyl)-6-(3,4,5- trimethoxyphenyl)-3(Z)-hexen-1,5-diyne (8) demonstrated the greatest growth inhibition activity. Compound 8 also arrested cancer cells in the G2/M phase and induced apoptosis via activation of Caspase-3. In addition to the G2/M block, compound 8 caused microtubule depolymerization at low concentrations and markedly decreased tumor size in xenographic studies.
AB - A series of novel enediyne-containing molecules, 1-aryl-6-(3,4,5- trimethoxyphenyl)-3(Z)-hexen-1,5-diynes, were synthesized and displayed significant IC50 values of 10-7 to 10-6 M against various cancer cell lines. Of these compounds, 1-(2-pyridinyl)-6-(3,4,5- trimethoxyphenyl)-3(Z)-hexen-1,5-diyne (8) demonstrated the greatest growth inhibition activity. Compound 8 also arrested cancer cells in the G2/M phase and induced apoptosis via activation of Caspase-3. In addition to the G2/M block, compound 8 caused microtubule depolymerization at low concentrations and markedly decreased tumor size in xenographic studies.
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U2 - 10.1016/j.ejmech.2013.01.011
DO - 10.1016/j.ejmech.2013.01.011
M3 - Article
C2 - 23419737
AN - SCOPUS:84873738478
VL - 62
SP - 526
EP - 533
JO - CHIM.THER.
JF - CHIM.THER.
SN - 0223-5234
ER -