引用本文:
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.
doi:
10.1016/j.cclet.2008.12.057
Citation: 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. doi: 10.1016/j.cclet.2008.12.057
Citation: 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. doi: 10.1016/j.cclet.2008.12.057
Design,synthesis and anti-HBV activity of novel bis(trifluoroethyl)phosphonomethyl ether derivatives of acyclovir
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 mmol/L was 33 times more potent than acyclovir with IC50 value of 100 mmol/L.
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关键词:
- Acyclovir
- / Phosphonate
- / Anti-HBV activity
English
Design,synthesis and anti-HBV activity of novel bis(trifluoroethyl)phosphonomethyl ether derivatives of acyclovir
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 IC50 value of 2.92 mmol/L was 33 times more potent than acyclovir with IC50 value of 100 mmol/L.
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Key words:
- Acyclovir
- / Phosphonate
- / Anti-HBV activity
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