| Design, synthesis and in vitro evaluation of L-amino acid esters prodrugs of acyclic nucleoside phosphonates as anti-HBV agent |
| |
| 引用本文： | Xiao Zhong Fu Sai Hong Jiang Jian Xin Yu She Yang RU Yun Ji. Design, synthesis and in vitro evaluation of L-amino acid esters prodrugs of acyclic nucleoside phosphonates as anti-HBV agent[J]. 中国化学快报, 2007, 18(7): 817-819. DOI: 10.1016/j.cclet.2007.05.013 |
| |
| 作者姓名： | Xiao Zhong Fu Sai Hong Jiang Jian Xin Yu She Yang RU Yun Ji |
| |
| 作者单位： | Xiao Zhong Fu a，Sai Hong Jiang b，Jian Xin c，Yu She Yang b，*，Ru Yun Ji b a School of Pharmacy，Guiyang Medical College，Guiyang 550004，China b State Key Laboratory of Drug Research，Shanghai Institute of Materia Medica，Shanghai Institute for Biological Sciences，Chinese Academy of Science，Shanghai 201203，China c Shanghai Fudan-Yueda Bio-Tech Co. Ltd.，Shanghai 201203，China |
| |
| 摘 要： | A series of novel L-amino acid esters prodrugs of acyclic nucleoside phosphonates was synthesized and their anti-HBVactivity was evaluated in HepG2 2.2.15 cells. Compound 1d exhibited more potent anti-HBV activity and lower cytotoxicity than those of adefovir dipivoxil with EC50 and CC50 values of 0.207 mmol/L and 2530 mmol/L, respectively.
|
| 关 键 词： | 脂肪族核苷膦酸酯 L-氨基酸 前体药物 抗-HBV活性 |
| 修稿时间： | 2007-01-08 |
Design, synthesis and in vitro evaluation of L-amino acid esters prodrugs of acyclic nucleoside phosphonates as anti-HBV agent |
| |
| Xiao Zhong Fu,Sai Hong Jiang,Jian Xin,Yu She Yang,Ru Yun Ji. Design, synthesis and in vitro evaluation of L-amino acid esters prodrugs of acyclic nucleoside phosphonates as anti-HBV agent[J]. Chinese Chemical Letters, 2007, 18(7): 817-819. DOI: 10.1016/j.cclet.2007.05.013 |
| |
| Authors: | Xiao Zhong Fu Sai Hong Jiang Jian Xin Yu She Yang Ru Yun Ji |
| |
| Affiliation: | 1. School of Pharmacy, Guiyang Medical College, Guiyang 550004, China;2. State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Shanghai Institute for Biological Sciences, Chinese Academy of Science, Shanghai 201203, China;3. Shanghai Fudan-Yueda Bio-Tech Co. Ltd., Shanghai 201203, China |
| |
| Abstract: | A series of novel L-amino acid esters prodrugs of acyclic nucleoside phosphonates was synthesized and their anti-HBVactivity was evaluated in HepG2 2.2.15 cells. Compound 1d exhibited more potent anti-HBV activity and lower cytotoxicity than those of adefovir dipivoxil with EC50 and CC50 values of 0.207 mmol/L and 2530 mmol/L, respectively. |
| |
| Keywords: | Acyclic nucleoside phosphonates L-Amino acid Prodrug Anti-HBV activity |
| 本文献已被 CNKI 维普 万方数据 ScienceDirect 等数据库收录！ |
