1-(2-((Z)-6-(2-(Trifluoromethyl)phenyl)hexa-3-en-1,5-diynyl)phenyl)piperidin-2-one as a new potent apoptosis agent.
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.
Tu
Yu-Sheng
YS
Faculty of Medicinal and Applied Chemistry, Kaohsiung Medical University, Kaohsiung, Taiwan.
Duh
Tsai-Hui
TH
Tseng
Chen-Yi
CY
Lin
Ying-Ting
YT
Lo
Yu-Hsiang
YH
Hu
Yi-Ling
YL
Chen
Chen-Hung
CH
Chien
Ching-Ming
CM
Yang
Sheng-Huei
SH
Lin
Shinne-Ren
SR
Yang
Shyh-Chyun
SC
Wu
Ming-Jung
MJ
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
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