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Synthesis, biological activity and structural study of new benzotriazole-based protein kinase CK2 inhibitors.

Título : Synthesis, biological activity and structural study of new benzotriazole-based protein kinase CK2 inhibitors.
Autor : Swider, R.
Pascual-Teresa Fernández, Beatriz de
Zapico Rodríguez, José María
Maslyk, Maciej
Materias: ProteínasAnálisis
Resumen : A new series of 4,5,6,7-tetrabromobenzotriazole (TBB) derivatives was synthesized and characterized as CK2 inhibitors. They were readily synthesized using a click chemistry approach based on a Cu(I)-catalyzed azide-alkyne 1,3-dipolar cycloaddition (CuAAC). Some of the synthesized compounds present interesting inhibitory activities using an in vitro assay, with Ki values in the low micro molar range and a high degree of selectivity against a panel of 24 kinases. Selected compounds were tested for their antiproliferative effect on several cancer cell lines, and for proapoptotic activity towards human Jurkat T-leukemia and MCF-7 breast adenocarcinoma cells, showing that they can be proposed as promising anticancer agents. Docking studies as well as crystallographic analysis allowed us to identify ligand –CK2 interactions that account for the molecular recognition process, and can help to further optimize this family of compounds as CK2 inhibitors.
Descripción : En: RSC Advances. ESSN. 2046-2069. 2015, 5, 72482
Financiado con cargo a proyectos de I+D nacional con referencias (CTQ2011-24741)
URI : http://hdl.handle.net/10637/8319
Derechos: http://creativecommons.org/licenses/by-nc-nd/4.0/deed.es
Fecha de publicación : 28-feb-2015
Centro : Universidad San Pablo-CEU
Aparece en las colecciones: Facultad de Farmacia





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