New benzimidazole derivatives as topoisomerase I inhibitors--synthesis and fluorometric analysis.

Katarzyna Błaszczak-Swiatkiewicz, Elzbieta Mikiciuk-Olasik

Department of Pharmaceutical Chemistry and Drug Analysis, Medical University, Łódź, Poland. katarzyna.blaszczak-swiatkiewicz@umed.lodz.pl

Acta poloniae pharmaceutica 2013 May-Jun

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A series of new benzimidazole derivatives with potential anticancer activity were tested as a new topoisomerase I inhibitors. The fluorometric method was used to determine in vitro the quantitative level of plasmid DNA relaxation by these compounds. Optimization of the fluorometric system and validation of the established analytical method were performed. Out of benzimidazole derivatives which were analyzed, in the case of five derivatives inhibition of topoisomerase I was greater than camptothecin (compounds 11, 12, 15, 21, 22).

Citation

Katarzyna Błaszczak-Swiatkiewicz, Elzbieta Mikiciuk-Olasik. New benzimidazole derivatives as topoisomerase I inhibitors--synthesis and fluorometric analysis. Acta poloniae pharmaceutica. 2013 May-Jun;70(3):451-8