New approaches to the synthesis of sildenafil analogues and their enzyme inhibitory activity

0446637 - ÚEB 2016 RIV GB eng J - Článek v odborném periodiku
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
Grant CEP: GA ČR GAP305/12/0783
Grant ostatní: GA MŠk(CZ) ED0007/01/01
Program: ED
Institucionální podpora: RVO:61389030
Klíčová slova: Sildenafil analogues * Pyrazolo[4,3-e][1,2,4] triazine * Sulfonamides
Kód oboru RIV: CE - Biochemie
Impakt faktor: 2.923, rok: 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.
Trvalý link: http://hdl.handle.net/11104/0248606