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New approaches to the synthesis of sildenafil analogues and their enzyme inhibitory activity
- 1.0446637 - ÚEB 2016 RIV GB eng J - Journal Article
Mojzych, M. - Karczmarzyk, Z. - Wysocki, W. - Ceruso, M. - Supuran, C.T. - Kryštof, Vladimír - Urbanczyk-Lipkowska, Z. - Kalicki, P.
New approaches to the synthesis of sildenafil analogues and their enzyme inhibitory activity.
Bioorganic & Medicinal Chemistry. Roč. 23, č. 7 (2015), s. 1421-1429. ISSN 0968-0896. E-ISSN 1464-3391
R&D Projects: GA ČR GAP305/12/0783
Grant - others:GA MŠk(CZ) ED0007/01/01
Program: ED
Institutional support: RVO:61389030
Keywords : Sildenafil analogues * Pyrazolo[4,3-e][1,2,4] triazine * Sulfonamides
Subject RIV: CE - Biochemistry
Impact factor: 2.923, year: 2015
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.
Permanent Link: http://hdl.handle.net/11104/0248606
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