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

作者：Mojzych Mariusz^*; Karczmarzyk Zbigniew; Wysocki Waldemar; Ceruso Mariangela; Supuran Claudiu T; Krystof Vladimir; Urbanczyk Lipkowska Zofia; Kalicki Przemyslaw

来源：Bioorganic & Medicinal Chemistry, 2015, 23(7): 1421-1429.

DOI：10.1016/j.bmc.2015.02.026

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

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.

• 出版日期2015-4-1