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

被引：9

作者：

Fu, Xiao Zhong ^{[2
]}

Ou, Yu ^{[2
]}

Xin, Jan ^{[3
]}

Yang, Yu She ^{[1
]}

机构：

[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

来源：

CHINESE CHEMICAL LETTERS | 2011年 / 22卷 / 12期

基金：

中国国家自然科学基金;

关键词：

Acyclic nucleoside phosphonates; L-Amino acid; Prodrug; INTRACELLULAR DELIVERY; DERIVATIVES; MCC-478; PMEA;

D O I：

10.1016/j.cclet.2011.09.005

中图分类号：

O6 [化学];

学科分类号：

0703 ;

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 EC50 and CC50 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.

引用

页码：1387 / 1390

页数：4

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