2. Academic Validation
  3. Synthesis and kinase inhibitory activity of new sulfonamide derivatives of pyrazolo[4,3-e][1,2,4]triazines

Synthesis and kinase inhibitory activity of new sulfonamide derivatives of pyrazolo[4,3-e][1,2,4]triazines

  • Eur J Med Chem. 2014 May 6:78:217-24. doi: 10.1016/j.ejmech.2014.03.054.
Mariusz Mojzych 1,  Veronika Šubertová 2,  Anna Bielawska 3,  Krzysztof Bielawski 3,  Václav Bazgier 2,  Karel Berka 4,  Tomáš Gucký 2,  Emilia Fornal 5,  Vladimír Kryštof 6
Affiliations

Affiliations

  • 1 Department of Chemistry, Siedlce University of Natural Sciences and Humanities, ul. 3 Maja 54, Siedlce 08-110, Poland.
  • 2 Centre of the Region Haná for Biotechnological and Agricultural Research, Laboratory of Growth Regulators, Faculty of Science, Palacký University, Šlechtitelů 11, 783 71 Olomouc, Czech Republic.
  • 3 Department of Medicinal Chemistry and Drug Technology, Medical University of Bialystok, Bialystok, Poland.
  • 4 Regional Centre of Advanced Technologies and Materials, Department of Physical Chemistry, Faculty of Science, Palacky University Olomouc, 17. listopadu 12, 77146 Olomouc, Czech Republic.
  • 5 Department of Chemistry, Laboratory of Separation and Spectroscopic Method Applications, Center for Interdisciplinary Research, The John Paul II Catholic University of Lublin, al. Krasnicka 102, 20-718 Lublin, Poland.
  • 6 Centre of the Region Haná for Biotechnological and Agricultural Research, Laboratory of Growth Regulators, Faculty of Science, Palacký University, Šlechtitelů 11, 783 71 Olomouc, Czech Republic. Electronic address: vladimir.krystof@upol.cz.
PMID: 24681986 DOI: 10.1016/j.ejmech.2014.03.054
Abstract

A new series of sulfonamide derivatives of pyrazolo[4,3-e][1,2,4]triazine has been synthesized and characterized. Their Anticancer activity was tested in vitro against multiple human Cancer cell lines and were found to have dose-dependent antiproliferative effects. Furthermore, some of the new compounds inhibited the Abl protein kinase with low micromolar IC50 values and exhibited selective activity against the Bcr-Abl positive K562 and BV173 cell lines, providing starting points for the further development of this new kinase inhibitor scaffold.

Keywords

Bcr-Abl; Cancer; Inhibitor; Kinase; Leukaemia; Pyrazolo[4,3-e][1,2,4]triazine; Synthesis.

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