Design, synthesis and in vitro evaluation of mono (2, 2, 2-trifluoroethyl) esters, mono L-amino acid ester prodrugs of acyclic nucleoside phosphonates as anti-HBV agents
文献类型：期刊论文
| 作者 | Fu, Xiao Zhong2; Ou, Yu2; Xin, Jan3; Yang, Yu She1 |
| 刊名 | CHINESE CHEMICAL LETTERS
 |
| 出版日期 | 2011-12 |
| 卷号 | 22期号:12页码:1387-1390 |
| 关键词 | Acyclic nucleoside phosphonates L-Amino acid Prodrug |
| ISSN号 | 1001-8417 |
| DOI | 10.1016/j.cclet.2011.09.005 |
| 文献子类 | Article |
| 英文摘要 | A series of novel mono (2, 2, 2-trifluoroethyl) esters, mono L-amino acid ester prodrugs of acyclic nucleoside phosphonates was synthesized and their in vitro anti-HBVactivity was evaluated in HepG 2 2.2.15 cells. Compound 1d exhibited more potent anti-HBV activity and lower cytotoxicity than those of adefovir dipivoxil and alamifovir (MCC-478) with EC(50) and CC(50) values of 0.01 mu mol/L and >8000 mu mol/L respectively. (C) 2011 Yu She Yang. Published by Elsevier B.V. on behalf of Chinese Chemical Society. All rights reserved. |
| WOS关键词 | CHRONIC HEPATITIS-B ; INTRACELLULAR DELIVERY ; DERIVATIVES ; MCC-478 ; VIRUS ; PMEA |
| 资助项目 | National Natural Science Foundation of China[20962004] ; Provincial Social Development Foundation of Guizhou, China[QKHSYZ [2009] ; Provincial Special Assistant Foundation for High-level Talents of Guizhou, China[TZJF-2009-36] ; Science and Technology Foundation of Guizhou Province, China[QKHJZ [2008] |
| WOS研究方向 | Chemistry |
| 语种 | 英语 |
| CSCD记录号 | CSCD:4376932 |
| WOS记录号 | WOS:000297186100001 |
| 出版者 | ELSEVIER SCIENCE INC |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/278320]  |
| 专题 | 药物化学研究室 中科院受体结构与功能重点实验室 新药研究国家重点实验室 |
| 通讯作者 | Yang, Yu She |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai Inst Biol Sci, State Key Lab Drug Res, Shanghai 201203, Peoples R China; 2.Guiyang Med Coll, Sch Pharm, Guiyang 550004, Peoples R China; 3.Shanghai Fudan Yueda Biotech Co Ltd, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Fu, Xiao Zhong,Ou, Yu,Xin, Jan,et al. Design, synthesis and in vitro evaluation of mono (2, 2, 2-trifluoroethyl) esters, mono L-amino acid ester prodrugs of acyclic nucleoside phosphonates as anti-HBV agents[J]. CHINESE CHEMICAL LETTERS,2011,22(12):1387-1390. |
| APA | Fu, Xiao Zhong,Ou, Yu,Xin, Jan,&Yang, Yu She.(2011).Design, synthesis and in vitro evaluation of mono (2, 2, 2-trifluoroethyl) esters, mono L-amino acid ester prodrugs of acyclic nucleoside phosphonates as anti-HBV agents.CHINESE CHEMICAL LETTERS,22(12),1387-1390. |
| MLA | Fu, Xiao Zhong,et al."Design, synthesis and in vitro evaluation of mono (2, 2, 2-trifluoroethyl) esters, mono L-amino acid ester prodrugs of acyclic nucleoside phosphonates as anti-HBV agents".CHINESE CHEMICAL LETTERS 22.12(2011):1387-1390. |
入库方式： OAI收割
来源：上海药物研究所
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