Author/Authors :
Yu-Sheng Tu، نويسنده , , Tsai-Hui Duh، نويسنده , , Chen-Yi Tseng، نويسنده , , Ying-Ting Lin، نويسنده , , Yu-Hsiang Lo، نويسنده , , Yi-Ling Hu، نويسنده , , Chen-Hung Chen، نويسنده , , Ching-Ming Chien، نويسنده , , Sheng-Huei Yang، نويسنده , , Shinne-Ren Lin، نويسنده , , Shyh-Chyun Yang، نويسنده , , Ming-Jung Wu، نويسنده ,
Abstract :
Compounds 4a–f, 5a–f and 6–9, showed significant growth inhibition activity against human tumor cell lines. Of these compounds, 1-(2-((Z)-6-(2-(trifluoromethyl)phenyl)hexa-3-en-1,5-diynyl)phenyl)piperidin-2-one (8) displayed the most potent growth inhibition activity. Compound 8 also arrested cancer cells in G2/M phase and induced apoptosis via activation of caspase-3 and -9. According to western-blotting analysis, compound 8 can up-regulate Bax, down-regulate Bcl-2 and XIAP, as well as promote cytochrome c release.
Keywords :
Acyclic enediynes , antitubulin , Apotosis , Antitumor agents
