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Bioorg Med Chem ; 17(21): 7412-7, 2009 Nov 01.
Article in English | MEDLINE | ID: mdl-19818634

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.


Subject(s)
Antineoplastic Agents/chemistry , Apoptosis , Piperidones/chemistry , Tubulin Modulators/chemistry , Antineoplastic Agents/chemical synthesis , Antineoplastic Agents/pharmacology , Caspase 3/metabolism , Cell Division , Cell Line, Tumor , Cytochromes c/metabolism , Drug Screening Assays, Antitumor , G2 Phase , HeLa Cells , Humans , Piperidones/chemical synthesis , Piperidones/pharmacology , Proto-Oncogene Proteins c-bcl-2/metabolism , Tubulin Modulators/chemical synthesis , Tubulin Modulators/pharmacology , bcl-2-Associated X Protein/metabolism
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