Design and synthesis of novel bis(L-amino acid) ester prodrugs of 9-[2-(phosphonomethoxy)ethyl] adenine (PMEA) with improved anti-HBV activity
文献类型：期刊论文
| 作者 | Fu, Xiaozhong; Jiang, Saihong; Li, Chuan; Xin, Jian; Yang, Yushe ; Ji, Ruyun
|
| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
 |
| 出版日期 | 2007-01-15 |
| 卷号 | 17期号:2页码:465-470 |
| 关键词 | adefovir anti-HBV nucleotide amino acid prodrug |
| ISSN号 | 0960-894X |
| DOI | 10.1016/j.bmcl.2006.10.021 |
| 文献子类 | Article |
| 英文摘要 | A series of novel biS(L-amino acid) ester prodrugs of 9-[2-(phosphonomethoxy)ethyl] adenine (PMEA) was synthesized and their anti-HBV activity was evaluated in HepG 2 2.2.15 cells. Compounds 11, 12, 21, 22, 26, and 27 demonstrated more potent anti-HBV activity and higher selective index (SI) than adefovir dipivoxil, which was used as a positive control. Compound 11, which was found to be the most potent one, was five times more potent than adefovir dipivoxil with EC50 value of 0.095 mu M and CC50 value of 6636 mu M. The SI value (> 69,000) of compound 11 was 60 times and 24 times higher than those of adefovir dipivoxil and lamivudine, respectively. In vitro stability studies showed that compound 11 was relatively more stable than adefovir dipivoxil with t(1/2) of 270 min. These findings suggested that compound 11 could be considered as a promising candidate for further in vivo studies. (c) 2006 Elsevier Ltd. All rights reserved. |
| WOS研究方向 | Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000244012200035 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/273355]  |
| 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, Yushe |
| 作者单位 | 1.Shanghai Fudan Yueda Biotech Co Ltd, Shanghai 201203, Peoples R China 2.Chinese Acad Sci, Shanghai Inst Biol Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Fu, Xiaozhong,Jiang, Saihong,Li, Chuan,et al. Design and synthesis of novel bis(L-amino acid) ester prodrugs of 9-[2-(phosphonomethoxy)ethyl] adenine (PMEA) with improved anti-HBV activity[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2007,17(2):465-470. |
| APA | Fu, Xiaozhong,Jiang, Saihong,Li, Chuan,Xin, Jian,Yang, Yushe,&Ji, Ruyun.(2007).Design and synthesis of novel bis(L-amino acid) ester prodrugs of 9-[2-(phosphonomethoxy)ethyl] adenine (PMEA) with improved anti-HBV activity.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,17(2),465-470. |
| MLA | Fu, Xiaozhong,et al."Design and synthesis of novel bis(L-amino acid) ester prodrugs of 9-[2-(phosphonomethoxy)ethyl] adenine (PMEA) with improved anti-HBV activity".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 17.2(2007):465-470. |
入库方式： OAI收割
来源：上海药物研究所
浏览0
下载0
收藏0
其他版本
除非特别说明，本系统中所有内容都受版权保护，并保留所有权利。