title: 1-(2-((Z)-6-(2-(Trifluoromethyl)phenyl)hexa-3-en-1,5-diynyl)phenyl)piperidin-2-one as a new potent apoptosis agent.
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.
authors.affiliation: Faculty of Medicinal and Applied Chemistry, Kaohsiung Medical University, Kaohsiung, Taiwan.
authors.forename: Yu-Sheng
authors.initials: YS
authors.lastname: Tu
authors.forename: Tsai-Hui
authors.initials: TH
authors.lastname: Duh
authors.forename: Chen-Yi
authors.initials: CY
authors.lastname: Tseng
authors.forename: Ying-Ting
authors.initials: YT
authors.lastname: Lin
authors.forename: Yu-Hsiang
authors.initials: YH
authors.lastname: Lo
authors.forename: Yi-Ling
authors.initials: YL
authors.lastname: Hu
authors.forename: Chen-Hung
authors.initials: CH
authors.lastname: Chen
authors.forename: Ching-Ming
authors.initials: CM
authors.lastname: Chien
authors.forename: Sheng-Huei
authors.initials: SH
authors.lastname: Yang
authors.forename: Shinne-Ren
authors.initials: SR
authors.lastname: Lin
authors.forename: Shyh-Chyun
authors.initials: SC
authors.lastname: Yang
authors.forename: Ming-Jung
authors.initials: MJ
authors.lastname: Wu
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D017209:Apoptosis; D053148:Caspase 3 / Q000378:metabolism; D002455:Cell Division; D045744:Cell Line, Tumor; D045304:Cytochromes c / Q000378:metabolism; D004354:Drug Screening Assays, Antitumor; D016195:G2 Phase; D006367:HeLa Cells; D006801:Humans; D010881:Piperidones / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D019253:Proto-Oncogene Proteins c-bcl-2 / Q000378:metabolism; D050257:Tubulin Modulators / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D051028:bcl-2-Associated X Protein / Q000378:metabolism
chemical_list: C545767:1-(2-((Z)-6-(2-(trifluoromethyl)phenyl)hexa-3-en-1,5-diynyl)phenyl)piperidin-2-one; D000970:Antineoplastic Agents; D010881:Piperidones; D019253:Proto-Oncogene Proteins c-bcl-2; D050257:Tubulin Modulators; D051028:bcl-2-Associated X Protein; D045304:Cytochromes c; D053148:Caspase 3