Cytostatic 6-arylpurine nucleosides. 6. SAR in anti-HCV and cytostatic activity of extended series of 6-hetarylpurine ribonucleosides
Language English Country United States Media print
Document type Journal Article, Research Support, Non-U.S. Gov't
PubMed
16134952
DOI
10.1021/jm050335x
Knihovny.cz E-resources
- MeSH
- Antiviral Agents chemical synthesis chemistry pharmacology MeSH
- Hepacivirus drug effects MeSH
- Humans MeSH
- Mice MeSH
- Cell Line, Tumor MeSH
- Antineoplastic Agents chemical synthesis chemistry pharmacology MeSH
- Purine Nucleosides chemical synthesis chemistry pharmacology MeSH
- Ribonucleosides chemical synthesis chemistry pharmacology MeSH
- Drug Screening Assays, Antitumor MeSH
- Structure-Activity Relationship MeSH
- Animals MeSH
- Check Tag
- Humans MeSH
- Mice MeSH
- Animals MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
- Names of Substances
- Antiviral Agents MeSH
- Antineoplastic Agents MeSH
- Purine Nucleosides MeSH
- Ribonucleosides MeSH
Significant anti-HCV activity of 6-hetarylpurine ribonucleosides has been discovered and is reported here for the first time and compared with cytostatic effect. An extended series of 6-hetarylpurine nucleosides has been prepared by heterocyclizations in position 6 of purine nucleosides or by cross-couplings of 6-chloropurine nucleosides with hetarylboronic acids, -stannanes, or -zinc halides. The most anti-HCV active were purine ribonucleosides bearing pyrrol-3-yl or 2-furyl groups exerting EC(90) = 0.14 and 0.4 microM, respectively.
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