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Tricyclic 2'-C-modified nucleosides as potential anti-HCV therapeutics.

ABSTRACT: Promising biological activity in a number of therapeutic areas has been reported for both tricyclic nucleosides and 2'-modified nucleosides. In particular, disubstitution at the C-2' position of nucleosides has resulted in significant activity against the hepatitis C virus (HCV). Combining this with the observation that tricyclic nucleosides developed in our laboratory have been shown to inhibit the RNA-dependent RNA polymerase NS5B led to the design of a series of 2'-modified tricyclic nucleosides. Details of the synthesis, structural characterization, and preliminary biological results are reported.

SUBMITTER: Wauchope OR

PROVIDER: S-EPMC2975515 | biostudies-literature | 2010 Oct

REPOSITORIES: biostudies-literature

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Tricyclic 2'-C-modified nucleosides as potential anti-HCV therapeutics.

Wauchope Orrette R OR Tomney Matthew J MJ Pepper Joseph L JL Korba Brent E BE Seley-Radtke Katherine L KL

Organic letters 20101001 20

Promising biological activity in a number of therapeutic areas has been reported for both tricyclic nucleosides and 2'-modified nucleosides. In particular, disubstitution at the C-2' position of nucleosides has resulted in significant activity against the hepatitis C virus (HCV). Combining this with the observation that tricyclic nucleosides developed in our laboratory have been shown to inhibit the RNA-dependent RNA polymerase NS5B led to the design of a series of 2'-modified tricyclic nucleosi ...[more]

PMID: 20845910

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