Design,synthesis and in vitro evaluation of mono(2,2,2-trifluoroethyl)esters,mono L-amino acid ester

• 出 处: Chinese Chemical Letters
• 发表日期: 2011年12期
• 关键词: nucleoside esters potent analogues moiety cytotoxicity alkyl methoxy afford subs

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 0.01μmol/L and >8000μmol/L respectively.

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-HBV activity was evaluated in HepG2 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.