Design, synthesis and in vitro evaluation of L-amino acid esters prodrugs of acyclic nucleoside phosphonates as anti-HBV agent  

作　　者：Xiao Zhong Fu Sai Hong Jiang Jian Xin Yu She Yang RU Yun Ji 

机构地区：[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

出　　处：《Chinese Chemical Letters》2007年第7期817-819,共3页中国化学快报（英文版）

摘　　要：A series of novel L-amino acid esters prodrugs of acyclic nucleoside phosphonates was synthesized and their anti-HBV activity 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 μmol/L and 2530 μmol/L, respectively.A series of novel L-amino acid esters prodrugs of acyclic nucleoside phosphonates was synthesized and their anti-HBV activity 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 μmol/L and 2530 μmol/L, respectively.

关 键 词：Acyclic nucleoside phosphonates L-Amino acid PRODRUG Anti-HBV activity 

分 类 号：R512.62[医药卫生—内科学] R914[医药卫生—临床医学]