title: Synthesis and kinase inhibitory activity of new sulfonamide derivatives of pyrazolo[4,3-e][1,2,4]triazines.
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.
authors.affiliation: Department of Chemistry, Siedlce University of Natural Sciences and Humanities, ul. 3 Maja 54, Siedlce 08-110, Poland.
authors.forename: Mariusz
authors.initials: M
authors.lastname: Mojzych
authors.affiliation: 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.
authors.forename: Veronika
authors.initials: V
authors.lastname: Šubertová
authors.affiliation: Department of Medicinal Chemistry and Drug Technology, Medical University of Bialystok, Bialystok, Poland.
authors.forename: Anna
authors.initials: A
authors.lastname: Bielawska
authors.affiliation: Department of Medicinal Chemistry and Drug Technology, Medical University of Bialystok, Bialystok, Poland.
authors.forename: Krzysztof
authors.initials: K
authors.lastname: Bielawski
authors.affiliation: 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.
authors.forename: Václav
authors.initials: V
authors.lastname: Bazgier
authors.affiliation: Regional Centre of Advanced Technologies and Materials, Department of Physical Chemistry, Faculty of Science, Palacky University Olomouc, 17. listopadu 12, 77146 Olomouc, Czech Republic.
authors.forename: Karel
authors.initials: K
authors.lastname: Berka
authors.affiliation: 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.
authors.forename: Tomáš
authors.initials: T
authors.lastname: Gucký
authors.affiliation: 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.
authors.forename: Emilia
authors.initials: E
authors.lastname: Fornal
authors.affiliation: 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.
authors.forename: Vladimír
authors.initials: V
authors.lastname: Kryštof
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D049109:Cell Proliferation / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D016044:Fusion Proteins, bcr-abl / Q000037:antagonists & inhibitors* / Q000378:metabolism; D018922:HL-60 Cells; D006801:Humans; D020014:K562 Cells; D061986:MCF-7 Cells; D015394:Molecular Structure; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D011720:Pyrazoles / Q000737:chemistry*; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D014227:Triazines / Q000737:chemistry*; D014407:Tumor Cells, Cultured
chemical_list: D000970:Antineoplastic Agents; D047428:Protein Kinase Inhibitors; D011720:Pyrazoles; D013449:Sulfonamides; D014227:Triazines; D016044:Fusion Proteins, bcr-abl
keywords: Bcr-Abl; Cancer; Inhibitor; Kinase; Leukaemia; Pyrazolo[4,3-e][1,2,4]triazine; Synthesis