| Design, synthesis and anti-HBV activity of novel bis（trifluoroethyl）phosphonomethyl ether derivatives of acyclovir |
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| 作者姓名： | Peng Lu Sai Hong Jiang Jiang Xia Liu Yu She Yang Ru Yun Ji |
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| 作者单位： | a State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Shanghai Institute for Biological Sciences, Chinese Academy of Science, Shanghai 201203, China;b Fudan University, Shanghai 200032, China |
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| 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 IC_(50)value of 2.92μmol/L was 33 times more potent than acyclovir with IC_(50)value of 100μmol/L.
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| 关 键 词： | 阿昔洛韦 活性评价 乙型肝炎病毒 衍生物 三氟 合成 设计 醚 |
| 收稿时间： | 10 November 2008 |
Design,synthesis and anti-HBV activity of novel bis(trifluoroethyl)phosphonomethyl ether derivatives of acyclovir |
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| Peng Lu,Sai Hong Jiang,Jiang Xia Liu,Yu She Yang,Ru Yun Ji.Design,synthesis and anti-HBV activity of novel bis(trifluoroethyl)phosphonomethyl ether derivatives of acyclovir[J].Chinese Chemical Letters,2009,20(5):507-510. |
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| Authors: | Peng Lua Sai Hong Jianga Jiang Xia Liub Yu She Yang Ru Yun Jia a State Key Laboratory of Drug Research |
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| Institution: | a State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Shanghai Institute for Biological Sciences, Chinese Academy of Science, Shanghai 201203, China;b Fudan University, Shanghai 200032, China |
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| Abstract: | 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 IC5o value of 2.92μmol/L was 33 times more potent than acyclovir with IC50 value of 100 μmol/L, |
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| Keywords: | Aeyclovir Phosphonate Anti-HBV activity |
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