New approaches to the synthesis of sildenafil analogues and their enzyme inhibitory activity
Language English Country England, Great Britain Media print-electronic
Document type Journal Article, Research Support, Non-U.S. Gov't
PubMed
25757603
DOI
10.1016/j.bmc.2015.02.026
PII: S0968-0896(15)00120-0
Knihovny.cz E-resources
- Keywords
- DFT calculations, Pyrazolo[4,3-e][1,2,4]triazine, Sildenafil analogues, Sulfonamides, X-ray structure analysis,
- MeSH
- K562 Cells MeSH
- Enzyme Inhibitors chemical synthesis MeSH
- Phosphodiesterase 5 Inhibitors chemical synthesis MeSH
- Crystallography, X-Ray MeSH
- Humans MeSH
- MCF-7 Cells MeSH
- Sildenafil Citrate analogs & derivatives chemical synthesis MeSH
- Check Tag
- Humans MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
- Names of Substances
- Enzyme Inhibitors MeSH
- Phosphodiesterase 5 Inhibitors MeSH
- Sildenafil Citrate MeSH
In the search for new biologically active chemotypes, several sildenafil analogs were prepared and characterized. The presence of the pyrazolo[4,3-e][1,2,4]triazine core is thought to be of interest for the enzyme inhibitory activity of these compounds. The designed derivatives incorporating the sildenafil scaffold were assayed as carbonic anhydrase inhibitors, and for their cytotoxic activity against MCF-7 and K562 cell lines. The X-ray analysis of one of these model compounds was performed and its crystal structure is described/compared to that of sildenafil.
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