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

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

  • Bioorg Med Chem. 2015 Apr 1;23(7):1421-9. doi: 10.1016/j.bmc.2015.02.026.
Mariusz Mojzych 1,  Zbigniew Karczmarzyk 2,  Waldemar Wysocki 2,  Mariangela Ceruso 3,  Claudiu T Supuran 4,  Vladimir Kryštof 5,  Zofia Urbańczyk-Lipkowska 6,  Przemysław Kalicki 7
Affiliations

Affiliations

  • 1 Department of Chemistry, Siedlce University of Natural Sciences and Humanities, 3 Maja 54, 08-110 Siedlce, Poland. Electronic address: mmojzych@yahoo.com.
  • 2 Department of Chemistry, Siedlce University of Natural Sciences and Humanities, 3 Maja 54, 08-110 Siedlce, Poland.
  • 3 Università degli Studi di Firenze, Polo Scientifico, Laboratorio di Chimica Bioinorganica, Rm. 188, Via della Lastruccia 3, 50019 Sesto Fiorentino, Florence, Italy.
  • 4 Università degli Studi di Firenze, Polo Scientifico, Laboratorio di Chimica Bioinorganica, Rm. 188, Via della Lastruccia 3, 50019 Sesto Fiorentino, Florence, Italy; Università degli Studi di Firenze, NEUROFARBA Department, Sezione di Scienze Farmaceutiche e Nutraceutiche, Via Ugo Schiff 6, 50019 Sesto Fiorentino, Florence, Italy. Electronic address: claudiu.supuran@unifi.it.
  • 5 Laboratory of Growth Regulators, Faculty of Science, Palacký University & Institute of Experimental Botany AS CR, Šlechtitelů 11, 78371 Olomouc, Czech Republic.
  • 6 Università degli Studi di Firenze, NEUROFARBA Department, Sezione di Scienze Farmaceutiche e Nutraceutiche, Via Ugo Schiff 6, 50019 Sesto Fiorentino, Florence, Italy.
  • 7 Institute of Organic Chemistry, Polish Academy of Sciences, Kasprzaka 44/52, 01-224 Warsaw, Poland.
PMID: 25757603 DOI: 10.1016/j.bmc.2015.02.026
Abstract

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.

Keywords

DFT calculations; Pyrazolo[4,3-e][1,2,4]triazine; Sildenafil analogues; Sulfonamides; X-ray structure analysis.

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