Synthesis, cytostatic, antimicrobial, and anti-HCV activity of 6-substituted 7-(het)aryl-7-deazapurine ribonucleosides
Language English Country United States Media print-electronic
Document type Journal Article, Research Support, Non-U.S. Gov't
PubMed
24397620
DOI
10.1021/jm4018948
Knihovny.cz E-resources
- MeSH
- Anti-Bacterial Agents chemical synthesis chemistry pharmacology MeSH
- Antitubercular Agents chemical synthesis chemistry pharmacology MeSH
- Antiviral Agents chemical synthesis chemistry pharmacology MeSH
- Cytostatic Agents chemical synthesis chemistry pharmacology MeSH
- Cytotoxins chemical synthesis chemistry pharmacology MeSH
- Hepacivirus drug effects physiology MeSH
- Humans MeSH
- Mycobacterium bovis drug effects MeSH
- Cell Line, Tumor MeSH
- Purine Nucleosides chemical synthesis chemistry pharmacology MeSH
- Virus Replication drug effects MeSH
- Ribonucleosides chemical synthesis chemistry pharmacology MeSH
- Structure-Activity Relationship MeSH
- Check Tag
- Humans MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
- Names of Substances
- Anti-Bacterial Agents MeSH
- Antitubercular Agents MeSH
- Antiviral Agents MeSH
- Cytostatic Agents MeSH
- Cytotoxins MeSH
- Purine Nucleosides MeSH
- Ribonucleosides MeSH
A series of 80 7-(het)aryl- and 7-ethynyl-7-deazapurine ribonucleosides bearing a methoxy, methylsulfanyl, methylamino, dimethylamino, methyl, or oxo group at position 6, or 2,6-disubstituted derivatives bearing a methyl or amino group at position 2, were prepared, and the biological activity of the compounds was studied and compared with that of the parent 7-(het)aryl-7-deazaadenosine series. Several of the compounds, in particular 6-substituted 7-deazapurine derivatives bearing a furyl or ethynyl group at position 7, were significantly cytotoxic at low nanomolar concentrations whereas most were much less potent or inactive. Promising activity was observed with some compounds against Mycobacterium bovis and also against hepatitis C virus in a replicon assay.
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