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

Bioorganic & Medicinal Chemistry
Mariusz MojzychPrzemysław Kalicki

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.

References

Aug 15, 1997·FEMS Microbiology Letters·V V SmirnovS A Dovjenko
Jan 3, 2008·Nature Reviews. Drug Discovery·Claudiu T Supuran

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Citations

Mar 24, 2015·Journal of Enzyme Inhibition and Medicinal Chemistry·Mariusz MojzychEmilia Fornal
May 23, 2017·Organic & Biomolecular Chemistry·Minghui ZhuHua Wang
Oct 1, 2015·Chemical Communications : Chem Comm·Haibo ZhuTao Tu
Oct 18, 2015·Scientia pharmaceutica·Ambati V Raghava ReddyAndra Naidu
Sep 3, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Zofia BernatMariusz Mojzych

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