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Published on: January 20, 2016
Aromatic analogues of DNA minor groove binders--synthesis and biological evaluation
Anna Pućkowska1, Krzysztof Bielawski, Anna Bielawska
1Department of Organic Chemistry, Medical University of Białystok, A. Mickiewicza 2a, 15-222 Białystok, Poland. pucanka@amb.edu.pl
Abstract:
Nine carbocyclic analogues of mono- and bis-lexitropsins and two analogues of pentamidine with unsubstituted N-terminal amine group were synthesized. We have investigated the cytotoxic activity of new aromatic analogues of DNA binding ligands in MCF-7 breast cancer cells and assessed their ability to act as inhibitors of topoisomerase I and II. These studies indicate that aromatic analogues of bis-netropsin contain two identical units tethered by alkyloxyl chains are a potent catalytic inhibitor of both topoisomerases and exhibit moderate cytotoxicity in MCF-7 breast cancer cells.
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