Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 78, Issue -, Pages 217-224Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2014.03.054
Keywords
Bcr-Abl; Kinase; Inhibitor; Synthesis; Cancer; Leukaemia; Pyrazolo[4,3-e][1,2,4]triazine
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Funding
- National Science Centre, Poland [NN405 092340]
- Czech Science Foundation [P305/12/0783]
- Centre of the Region Hand for Biotechnological Agricultural Research [ED0007/01/01]
- Palacky University [PrF_2014_023]
- Operational Program Research and Development for Innovations European Regional Development Fund [CZ.1.05/2.1.00/03.0058]
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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. (C) 2014 Elsevier Masson SAS. All rights reserved.
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