Aromatic analogues of DNA minor groove binders--synthesis and biological evaluation.


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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@article{Pukowska2004AromaticAO, title={Aromatic analogues of DNA minor groove binders--synthesis and biological evaluation.}, author={Anna Pu{\'c}kowska and Krzysztof Bielawski and Anna Kocoń - Bielawska and Krystyna Midura-Nowaczek}, journal={European journal of medicinal chemistry}, year={2004}, volume={39 1}, pages={99-105} }