Synthesis of polybrominated benzimidazole and benzotriazole derivatives containing a tetrazole ring and their cytotoxic activity
Edyta Łukowska-Chojnacka , Patrycja Wińska , Monika Wielechowska , Maria Bretner
AbstractA 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 (rhCK2a) 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.
|Journal series||Monatshefte Fur Chemie, ISSN 0026-9247|
|Publication size in sheets||0.5|
|Keywords in English||Antitumor agents; Azole; Benzimidazole Heterocycles; Tetrazole Total synthesis Int|
|Score|| = 20.0, 28-11-2017, ArticleFromJournal|
= 25.0, 28-11-2017, ArticleFromJournal
|Publication indicators||: 2016 = 1.282 (2) - 2016=1.224 (5)|
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