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

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    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
    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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