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
来源：
ORGANIC & BIOMOLECULAR CHEMISTRY | 2016年 / 14卷 / 37期
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.
引用
收藏
页码：8743 / 8757
页数：15
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