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New approaches to the synthesis of sildenafil analogues and their enzyme inhibitory activity
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SYSNO ASEP 0446637 Document Type J - Journal Article R&D Document Type Journal Article Subsidiary J Článek ve WOS Title New approaches to the synthesis of sildenafil analogues and their enzyme inhibitory activity Author(s) Mojzych, M. (PL)
Karczmarzyk, Z. (PL)
Wysocki, W. (PL)
Ceruso, M. (IT)
Supuran, C.T. (IT)
Kryštof, Vladimír (UEB-Q) RID, ORCID
Urbanczyk-Lipkowska, Z. (PL)
Kalicki, P. (PL)Source Title Bioorganic & Medicinal Chemistry. - : Elsevier - ISSN 0968-0896
Roč. 23, č. 7 (2015), s. 1421-1429Number of pages 9 s. Language eng - English Country GB - United Kingdom Keywords Sildenafil analogues ; Pyrazolo[4,3-e][1,2,4] triazine ; Sulfonamides Subject RIV CE - Biochemistry R&D Projects GAP305/12/0783 GA ČR - Czech Science Foundation (CSF) Institutional support UEB-Q - RVO:61389030 UT WOS 000350995500006 DOI 10.1016/j.bmc.2015.02.026 Annotation 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. Workplace Institute of Experimental Botany Contact David Klier, knihovna@ueb.cas.cz, Tel.: 220 390 469 Year of Publishing 2016
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