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

查看全文 作　　者：Xiao Zhong [1]Fu;Yu [1]Ou;Jan [2]Xin;Yu She [3]Yang

机构地区：[1]School of Pharmacy,Guiyang Medical College,Guiyang 550004,China;[2]Shanghai Fudan-Yueda Bio-Tech Co.,Ltd.,Shanghai 201203,China;[3]State Key Laboratory of Drug Research,Shanghai Institute of Materia Medica,Shanghai Institute for Biological Sciences, Chinese Academy of Science,Shanghai 201203,China

出　　处：《Chinese Chemical Letters》索引2011年第22卷第12期,共4页

基　　金：supported by the grants from the National Natural Science Foundation of China(No.20962004);the Provincial Social Development Foundation of Guizhou,China(No.QKHSYZ[2009]3081);Provincial Special Assistant Foundation for High-level Talents of Guizhou,China(No.TZJF-2009-36);Science and Technology Foundation of Guizhou Province,China(No.QKHJZ[2008]2140) 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 0.01μmol/L and >8000μmol/L respectively. 关键词：L-氨基酸酯药物合成膦酸酯乙型肝炎评价体外三氟核苷

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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

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