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Bifunctional aryloxyphosphoramidate prodrugs of 2′-C-Me-uridine: synthesis and anti-HCV activity
被引:4
作者:
Maiti, Munmun
[1
]
Gao, Ling-Jie
[1
]
Huang, Chunsheng
[2
]
Ptak, Roger G.
[2
]
Murray, Michael G.
[2
]
De Jonghe, Steven
[1
]
Herdewijn, Piet
[1
]
机构:
[1] Katholieke Univ Leuven, Rega Inst, Med Chem Lab, Minderbroedersstr 10, B-3000 Leuven, Belgium
[2] Southern Res, Infect Dis Res, 431 Aviat Way, Frederick, MD 21701 USA
基金:
美国国家卫生研究院;
关键词:
HEPATITIS-C VIRUS;
ARYLOXY PHOSPHORAMIDATE TRIESTERS;
NUCLEOSIDE PHOSPHATE;
AMINO-ACID;
REPLICATION;
TECHNOLOGY;
INHIBITORS;
CANCER;
CELLS;
D O I:
10.1039/c6ob01189f
中图分类号:
O62 [有机化学];
学科分类号:
070303 ;
081704 ;
摘要:
In an attempt to identify novel nucleoside phosphoramidate analogues for improving the anti-HCV activity of 2'-C-Me-uridine, we have synthesized for the first time a series of L-glutamic acid, L-serine, L-threonine and L-tyrosine containing aryloxyphosphoramidate prodrugs of 2'-C-Me-uridine. Evaluation of their activity against HCV revealed that they displayed very potent anti-HCV activity, with EC50 values that are in the same range as of Sofosbuvir.
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页码:8743 / 8757
页数:15
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