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    题名: Synthesis and biological evaluation of peptidyl organotrifluoroborates and their corresponding boron analogs
    作者: Tsai, Chia-Hua;Lin, Chia-Hung;Hsieh, Ching-Tien;Cai, Chih-Cheng;Lin, Ting-Ju;Liu, Pin-Yi;Lin, Meng-Hsuan;Wu, Meng-Ju;Fu, Chia-Chieh;Wu, Yang-Chang;Chang, Fnag-Rong;Pan, Po-Shen
    贡献者: 淡江大學化學學系
    关键词: Peptide;Boronic acid;Organotrifluoroborate;Potassium trifluoroborate;HepG2;MDA-MB231
    日期: 2014-07-01
    上传时间: 2014-08-08 14:45:22 (UTC+8)
    出版者: Springer Netherlands
    摘要: Six peptidyl organotrifluoroborates and their corresponding boronate esters and/or boronic acid analogs were designed and synthesized. Their anti-proliferative activity against hepatocellular carcinoma cells (HepG2) and human metastatic breast cancer cells (MDA-MB231) were evaluated by use of an MTT assay. Potassium {4-[(3S,6S,9S)-3,6-dibenzyl-9-isopropyl-4,7,10-trioxo-11-oxa-2,5,8-triazadodecyl]phenyl}trifluoroborate (B6) was potent (IC50 = 29.9 μM) against MDA-MB231, and {4-[(3S,6S,9S)-6-benzyl-3-((benzyloxy)methyl)-9-isopropyl-4,7,10-trioxo-11-oxa-2,5,8-triazadodecyl]phenyl}boronic acid (B9) and Potassium {4-[(3S,6S,9S)-6-benzyl-3-((benzyloxy)methyl)-9-isopropyl-4,7,10-trioxo-11-oxa-2,5,8-triazadodecyl]phenyl}trifluoroborate (B10) had broad anti-proliferative activity against HepG2 (IC50 = 24.7 and 21.8 μM, respectively) and MDA-MB231 (IC50 = 24.5 and 18.9 μM, respectively).
    關聯: Research on Chemical Intermediates 40(6), pp.2187-2198
    DOI: 10.1007/s11164-014-1596-7
    显示于类别:[化學學系暨研究所] 期刊論文

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