title: Synthesis of polybrominated benzimidazole and benzotriazole derivatives containing a tetrazole ring and their cytotoxic activity.
abstract: A series of new benzimidazole and benzotriazole derivatives containing a tetrazole moiety was synthesized byN-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.
authors.affiliation: Faculty of Chemistry, Institute of Biotechnology, Warsaw University of Technology, Noakowskiego St. 3, 00-664 Warsaw, Poland.
authors.forename: Edyta
authors.initials: E
authors.lastname: Łukowska-Chojnacka
authors.affiliation: Faculty of Chemistry, Institute of Biotechnology, Warsaw University of Technology, Noakowskiego St. 3, 00-664 Warsaw, Poland.
authors.forename: Patrycja
authors.initials: P
authors.lastname: Wińska
authors.affiliation: Faculty of Chemistry, Institute of Biotechnology, Warsaw University of Technology, Noakowskiego St. 3, 00-664 Warsaw, Poland.
authors.forename: Monika
authors.initials: M
authors.lastname: Wielechowska
authors.affiliation: Faculty of Chemistry, Institute of Biotechnology, Warsaw University of Technology, Noakowskiego St. 3, 00-664 Warsaw, Poland.
authors.forename: Maria
authors.initials: M
authors.lastname: Bretner
keywords: Antitumor agents; Azole; Benzimidazole; Heterocycles; Tetrazole; Total synthesis