Synthesis and biological evaluation of peptidyl organotrifluoroborates and their corresponding boron analogs
學年 102
學期 2
出版（發表）日期 2014-07-01
作品名稱 Synthesis and biological evaluation of peptidyl organotrifluoroborates and their corresponding boron analogs
作品名稱（其他語言）
著者 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
單位 淡江大學化學學系
出版者 Dordrecht: Springer Netherlands
著錄名稱、卷期、頁數 Research on Chemical Intermediates 40(6), pp.2187-2198
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).
關鍵字 Peptide;Boronic acid;Organotrifluoroborate;Potassium trifluoroborate;HepG2;MDA-MB231
語言 en
ISSN 0922-6168 1568-5675
期刊性質 國外
收錄於 SCI
產學合作
通訊作者 Pan, Po-Shen
審稿制度 是
國別 NLD
公開徵稿
出版型式 ,電子版,紙本
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