1-(2-((Z)-6-(2-(Trifluoromethyl)phenyl)hexa-3-en-1,5-diynyl)phenyl)piperidin-2-one as a new potent apoptosis agent |
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| Authors: | Yu-Sheng Tu Tsai-Hui Duh Chen-Yi Tseng Ying-Ting Lin Yu-Hsiang Lo Yi-Ling Hu Chen-Hung Chen Ching-Ming Chien Sheng-Huei Yang Shinne-Ren Lin Shyh-Chyun Yang Ming-Jung Wu |
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| Institution: | aFaculty of Medicinal and Applied Chemistry, Kaohsiung Medical University, Kaohsiung, Taiwan;bGraduate Institute of Pharmaceutical Sciences, Kaohsiung Medical University, Kaohsiung, Taiwan;cDepartment of Chemistry, National Sun Yat-sen University, Kaohsiung, Taiwan;dFaculty of Biotechnology, Kaohsiung Medical University, Kaohsiung, Taiwan |
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| 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. |
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| Keywords: | Acyclic enediynes Antitumor agents Antitubulin Apotosis |
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