Design,synthesis and anti-HBV activity of novel bis(trifluoroethyl)phosphonomethyl ether derivatives of acyclovir
Design,synthesis and anti-HBV activity of novel bis(trifluoroethyl)phosphonomethyl ether derivatives of acyclovir作者机构:State Key Laboratory of Drug Research Shanghai Institute of Materia Medica Shanghai Institute for Biological Sciences Chinese Academy of Science Shanghai 201203 China Fudan University Shanghai 200032 China
出 版 物:《Chinese Chemical Letters》 (中国化学快报(英文版))
年 卷 期:2009年第20卷第5期
页 面:507-510页
核心收录:
学科分类:1007[医学-药学(可授医学、理学学位)] 090403[农学-农药学(可授农学、理学学位)] 09[农学] 0904[农学-植物保护] 0703[理学-化学] 10[医学]
主 题:Acyclovir Phosphonate Anti-HBV activity
摘 要:A series of novel bis(trifluoroethyl)phosphonomethyl ether derivatives of acyclovir was synthesized and their in vitro anti-HBV activity was evaluated in HepG2 2.2.15 cells. In contrast to acyclovir, most of the described phosphonates emerged as potent inhibitors of HBV replication. Especially, the most active compound 11 with IC50 value of 2.92 μmol/L was 33 times more potent than acyclovir with ICso value of 100 μmol/L.