引用本文:
Xiao Zhong Fu, Yu Ou, Jan Xin, Yu She Yang. 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[J]. Chinese Chemical Letters,
2011, 22(12): 1387-1390.
doi:
10.1016/j.cclet.2011.09.005
Citation: Xiao Zhong Fu, Yu Ou, Jan Xin, Yu She Yang. 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[J]. Chinese Chemical Letters, 2011, 22(12): 1387-1390. doi: 10.1016/j.cclet.2011.09.005
Citation: Xiao Zhong Fu, Yu Ou, Jan Xin, Yu She Yang. 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[J]. Chinese Chemical Letters, 2011, 22(12): 1387-1390. doi: 10.1016/j.cclet.2011.09.005
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
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 EC50 and CC50 values of 0.01 μmol/L and >8000 μmol/L respectively.
English
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
Abstract:
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 EC50 and CC50 values of 0.01 μmol/L and >8000 μmol/L respectively.
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Key words:
- Acyclic nucleoside phosphonates
- / L-Amino acid
- / Prodrug
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