Journal
JOURNAL OF THE CHINESE CHEMICAL SOCIETY
Volume 55, Issue 3, Pages 668-674Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/jccs.200800100
Keywords
enediyne; antitumor; apoptosis
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Funding
- National Science Council of the Republic of China
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A series of 1-(6-(2-(2-arylethynyl)phenyl)hexyn-5-yl)piperidin-2-ones 2a-j were synthesized and their antitumor activities were evaluated. Of these compounds, 1-(6-(2-(2-(4-nitrophenyl)ethynyl)phenyl)hexyn-5 -yl)piperidin-2 -one (2j) showed the highest potency of growth inhibition activity, especially against the RPMI-8226 (0.4 mu M) and SR (0.02 mu M) cell lines of human leukemia. Compound 2j also induced significant apoptotic progress in the cell cycle assay with the K-562 cell line.
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