- 2'-FLUORO-4'-SUBSTITUTED NUCLEOSIDES, THE PREPARATION AND USE
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The present invention provides 2'-fluorine-4'-substituted-nucleoside analogues or their pro-drugs or 5'-phosphate esters (including the pro-drugs of the 5'-phosphate esters), preparation methods and uses thereof. The compounds have the general formula as follows: wherein: R = CH3, CH, N3, C≡CH; R' = H, F; X = F, OH, NH2; Y = H, CH3, F, OH, NH2 The compounds are used in the synthesis of drugs for the treatment of virus infection, especially for the treatment of HBV, HCV or HIV infection.
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Page/Page column 12
(2010/05/13)
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- Synthesis of some 2′-fluoro-2′-deoxy-3′-C-ethynyl and 3′-C-vinyl-β-D-lyxofuranosyl nucleosides
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1-(2-Fluoro-2-deoxy-β-D-arabinofuranosyl)uracil (5) and 1-(2-fluoro-2-deoxy-β-D-arabinofuranosyl)cytosine (6) were synthesized as reported earlier. Both of these compounds were converted into 2′-fluoro-2′-deoxy-3′-C-ethynyl and 3′-C-vinyl-β-D- lyxofuranosyl nucleosides (16-19) by a multistep sequence. All these new nucleosides were evaluated against seven human tumor cell lines in vitro. Copyright Taylor & Francis, Inc.
- Moukha-Chafiq,Tiwari,Secrist III
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p. 713 - 715
(2007/10/03)
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- Synthesis and anti-HIV-1 activity of 2'-'up'-fluoro analogues of active anti-AIDS nucleosides 3'-azido-3'-deoxythymidine (AZT) and 2',3'-dideoxycytidine (DDC)
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1-(3-Azido-2,3-dideoxy-2-fluoro-β-D-arabinofuranosyl)thymine (6, F-AZT) and 1-(2,3-dideoxy-2-fluoro-β-D-threopentofuranosyl)cytosine (12, F-DDC) were synthesized from the potent antiherpes virus nucleosides 1-(2-deoxy-2-fluoro-β-D-arabinofuranosyl)thymine
- Watanabe,Harada,Zeidler,Matulic-Adamic,Takahashi,Ren,Cheng,Fox,Chou,Zhu,Polsky,Gold,Armstrong
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p. 2145 - 2150
(2007/10/02)
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- Synthesis and antiviral activity of monofluoro and difluoro analogues of pyrimidine deoxyribonucleosides against human immunodeficiency virus (HIV-1)
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A range of 2'-fluoro and 2',3'-difluoro analogues of pyrimidine deoxyribonucleosides have been synthesized and evaluaed against human immunodeficiency virus (HIV-1) in a human lymphoblastoid cell line. Among these compounds, 1-(2,3-dideoxy-2-fluoro-β-D-threopentofuranosyl)cytosine (12), 2',3'-didehydro-2',3'-dideoxy-2'-fluorocytidine (35), 1-(2,3-dideoxy-2,3-difluoro-β-D-arabinofuranosyl)cytosine (41), and 3'-deoxy-2',3'-didehydro-2'-fluorothymidine (45) were found to have significant antiviral activity, with IC50 values of 0.65, 10, 10, and 100 μM, respectively. The structure-activity relationships are discussed.
- Martin,Bushnell,Duncan,Dunsdon,Hall,Machin,Merrett,Parkes,Roberts,Thomas,Galpin,Kinchington
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p. 2137 - 2145
(2007/10/02)
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