1133865-97-0Relevant academic research and scientific papers
Synthesis of polybrominated benzimidazole and benzotriazole derivatives containing a tetrazole ring and their cytotoxic activity
?ukowska-Chojnacka, Edyta,Wińska, Patrycja,Wielechowska, Monika,Bretner, Maria
, p. 1789 - 1796 (2016)
Abstract: A series of new benzimidazole and benzotriazole derivatives containing a tetrazole moiety was synthesized by N-alkylation of 5-aryltetrazole with 4,5,6,7-tetrabromo-1-(3-chloropropyl)-1H-benzimidazole and 4,5,6,7-tetrabromo-2-(3-chloropropyl)-2H-benzotriazole. The reaction was regioselective and mostly 2,5-disubstituted tetrazole derivatives were obtained. The effect of all synthesized compounds on human recombinant casein kinase 2alpha subunit (rhCK2α) and cytotoxicity against human T-cell lymphoblast (CCRF-CEM) and breast adenocarcinoma (MCF-7) cell lines were evaluated. The results have shown that many of the synthesized compounds exhibit significant cytotoxicity at micromolar concentration. Graphical abstract: [Figure not available: see fulltext.]
Synthesis of new analogs of benzotriazole, benzimidazole and phthalimide-potential inhibitors of human protein kinase CK2
Najda-Bernatowicz, Andzelika,Lebska, Maja,Orzeszko, Andrzej,Kopanska, Katarzyna,Krzywinska, Ewa,Muszynska, Grazyna,Bretner, Maria
experimental part, p. 1573 - 1578 (2009/08/08)
New derivatives of 4,5,6,7-tetrabromo-1H-1,2,3-benzotriazole (TBBt), 4,5,6,7-tetrabromo-1H-benzimidazole (TBBi), and N-substituted tetrabromophthalimides were synthesized and their effect on the activity of human protein kinase CK2 was examined. The most active were derivatives with N-hydroxypropyl substituents (IC50 in 0.32-0.54 μM range) whereas derivatives of phthalimide were almost ineffective.
