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Synthesis and biological evaluation of peptidyl organotrifluoroborates and their corresponding boron analogs |
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| Authors: | Chia-Hua Tsai Chia-Hung Lin Ching-Tien Hsieh Chih-Cheng Cai Ting-Ju Lin Pin-Yi Liu Meng-Hsuan Lin Meng-Ju Wu Chia-Chieh Fu Yang-Chang Wu Fang-Rong Chang Po-Shen Pan |
| Institution: | 1. Department of Chemistry, Tamkang University, No. 151 Yingzhuan Rd., Tamsui Dist., New Taipei City, 25137, Taiwan, ROC 2. Graduate Institute of Natural Products, Kaohsiung Medical University, 100 Shi-Chuan 1st Rd., Kaohsiung, 80708, Taiwan, ROC 3. Graduate Institute of Integrated Medicine, College of Chinese Medicine, China Medical University, Taichung, 404, Taiwan, ROC 4. Cancer Center, Kaohsiung Medical University Hospital, Kaohsiung, 807, Taiwan, ROC |
| 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). |
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