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
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...
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| Veröffentlicht in: | Chinese chemical letters 2011-12, Vol.22 (12), p.1387-1390 |
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| Hauptverfasser: | , , , |
| Format: | Artikel |
| Sprache: | eng |
| Schlagworte: | |
| Online-Zugang: | Volltext |
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| Zusammenfassung: | 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 EC
50 and CC
50 values of 0.01
μmol/L and >8000
μmol/L respectively. |
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| ISSN: | 1001-8417 1878-5964 |
| DOI: | 10.1016/j.cclet.2011.09.005 |