Literature DB >> 24681986

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

Mariusz Mojzych1, Veronika Šubertová2, Anna Bielawska3, Krzysztof Bielawski3, Václav Bazgier2, Karel Berka4, Tomáš Gucký2, Emilia Fornal5, Vladimír Kryštof6.   

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.
Copyright © 2014 Elsevier Masson SAS. All rights reserved.

Entities:  

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

Mesh：

Substances：

Year:  2014        PMID： 24681986     DOI： 10.1016/j.ejmech.2014.03.054

Source DB:  PubMed          Journal:  Eur J Med Chem        ISSN： 0223-5234            Impact factor:   6.514


  7 in total

1.  Preparation of Novel Pyrazolo[4,3-e]tetrazolo[1,5-b][1,2,4]triazine Sulfonamides and Their Experimental and Computational Biological Studies.

Authors:  Mateusz Kciuk; Somdutt Mujwar; Anna Szymanowska; Beata Marciniak; Karol Bukowski; Mariusz Mojzych; Renata Kontek
Journal:  Int J Mol Sci       Date:  2022-05-24       Impact factor: 6.208

2.  The Effect of Novel 7-methyl-5-phenyl-pyrazolo[4,3-e]tetrazolo[4,5-b][1,2,4]triazine Sulfonamide Derivatives on Apoptosis and Autophagy in DLD-1 and HT-29 Colon Cancer Cells.

Authors:  Agnieszka Gornowicz; Anna Szymanowska; Mariusz Mojzych; Krzysztof Bielawski; Anna Bielawska
Journal:  Int J Mol Sci       Date:  2020-07-23       Impact factor: 5.923

3.  Exploration of novel heterofused 1,2,4-triazine derivative in colorectal cancer.

Authors:  Justyna Magdalena Hermanowicz; Anna Szymanowska; Beata Sieklucka; Robert Czarnomysy; Krystyna Pawlak; Anna Bielawska; Krzysztof Bielawski; Joanna Kalafut; Alicja Przybyszewska; Arkadiusz Surazynski; Adolfo Rivero-Muller; Mariusz Mojzych; Dariusz Pawlak
Journal:  J Enzyme Inhib Med Chem       Date:  2021-12       Impact factor: 5.051

4.  Pyrazolo[4,3-e]tetrazolo[1,5-b][1,2,4]triazine Sulfonamides as Novel Potential Anticancer Agents: Cytotoxic and Genotoxic Activities In Vitro.

Authors:  Karol Bukowski; Beata Marciniak; Mateusz Kciuk; Mariusz Mojzych; Renata Kontek
Journal:  Molecules       Date:  2022-06-11       Impact factor: 4.927

5.  Synthesis, Structural Characterization, and Biological Activity of New Pyrazolo[4,3-e][1,2,4]triazine Acyclonucleosides.

Authors:  Mariusz Mojzych; Zofia Bernat; Zbigniew Karczmarzyk; Joanna Matysiak; Andrzej Fruziński
Journal:  Molecules       Date:  2020-01-05       Impact factor: 4.411

Review 6.  Review of the Synthesis and Anticancer Properties of Pyrazolo[4,3-e][1,2,4]triazine Derivatives.

Authors:  Zofia Bernat; Anna Szymanowska; Mateusz Kciuk; Katarzyna Kotwica-Mojzych; Mariusz Mojzych
Journal:  Molecules       Date:  2020-08-29       Impact factor: 4.411

Review 7.  Downfalls of Chemical Probes Acting at the Kinase ATP-Site: CK2 as a Case Study.

Authors:  Eleanor L Atkinson; Jessica Iegre; Paul D Brear; Elizabeth A Zhabina; Marko Hyvönen; David R Spring
Journal:  Molecules       Date:  2021-03-31       Impact factor: 4.411
  7 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.