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.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Antineoplastic Agents / chemical synthesis
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Antineoplastic Agents / chemistry*
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Antineoplastic Agents / pharmacology
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Apoptosis*
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Caspase 3 / metabolism
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Cell Division
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Cell Line, Tumor
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Cytochromes c / metabolism
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Drug Screening Assays, Antitumor
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G2 Phase
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HeLa Cells
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Humans
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Piperidones / chemical synthesis
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Piperidones / chemistry*
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Piperidones / pharmacology
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Proto-Oncogene Proteins c-bcl-2 / metabolism
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Tubulin Modulators / chemical synthesis
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Tubulin Modulators / chemistry*
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Tubulin Modulators / pharmacology
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bcl-2-Associated X Protein / metabolism
Substances
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1-(2-((Z)-6-(2-(trifluoromethyl)phenyl)hexa-3-en-1,5-diynyl)phenyl)piperidin-2-one
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Antineoplastic Agents
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Piperidones
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Proto-Oncogene Proteins c-bcl-2
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Tubulin Modulators
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bcl-2-Associated X Protein
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Cytochromes c
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Caspase 3