Synthesis and biological evaluation of peptidyl organotrifluoroborates and their corresponding boron analogs

doi:10.1007/s11164-014-1596-7

淡江大學機構典藏 > 理學院 > 化學學系暨研究所 > 期刊論文 > Item 987654321/98497

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Title:	Synthesis and biological evaluation of peptidyl organotrifluoroborates and their corresponding boron analogs
Authors:	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
Contributors:	淡江大學化學學系
Keywords:	Peptide;Boronic acid;Organotrifluoroborate;Potassium trifluoroborate;HepG2;MDA-MB231
Date:	2014-07-01
Issue Date:	2014-08-08 14:45:22 (UTC+8)
Publisher:	Springer Netherlands
Abstract:	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).
Relation:	Research on Chemical Intermediates 40(6), pp.2187-2198
DOI:	10.1007/s11164-014-1596-7
Appears in Collections:	[化學學系暨研究所] 期刊論文

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