New approaches to the synthesis of sildenafil analogues and their enzyme inhibitory activity
Jazyk angličtina Země Anglie, Velká Británie Médium print-electronic
Typ dokumentu časopisecké články, práce podpořená grantem
PubMed
25757603
DOI
10.1016/j.bmc.2015.02.026
PII: S0968-0896(15)00120-0
Knihovny.cz E-zdroje
- Klíčová slova
- DFT calculations, Pyrazolo[4,3-e][1,2,4]triazine, Sildenafil analogues, Sulfonamides, X-ray structure analysis,
- MeSH
- buňky K562 MeSH
- inhibitory enzymů chemická syntéza MeSH
- inhibitory fosfodiesterasy 5 chemická syntéza MeSH
- krystalografie rentgenová MeSH
- lidé MeSH
- MFC-7 buňky MeSH
- sildenafil citrát analogy a deriváty chemická syntéza MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
- Názvy látek
- inhibitory enzymů MeSH
- inhibitory fosfodiesterasy 5 MeSH
- sildenafil citrát 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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