In vitro anticancer activity and evaluation of DNA duplex binding affinity of phenyl-substituted indoloquinolines |
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Authors: | Riechert-Krause Fanny Eick Andrea Grünert Renate Bednarski Patrick J Weisz Klaus |
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Institution: | a Institute of Biochemistry, Ernst-Moritz-Arndt University of Greifswald, Felix-Hausdorff-Strasse 4, D-17487 Greifswald, Germany b Department of Pharmaceutical and Medicinal Chemistry, Institute of Pharmacy, Ernst-Moritz-Arndt University of Greifswald, Friedrich-Ludwig-Jahn-Strasse 17, D-17487 Greifswald, Germany |
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Abstract: | Phenyl-substituted indoloquinolines were studied for their biological activity and their DNA binding affinity. Water-soluble aminoalkyl derivatives were prepared and have shown significant in vitro anticancer activity. Unlike previous reports on the potential role of duplex DNA as target for various indoloquinoline based drugs, duplex UV melting experiments and fluorescence titrations suggest only weak and moderately strong binding of the phenyl-substituted indoloquinolines at 120 mM and 20 mM Na+ concentrations, respectively. Binding is suggested by ethidium displacement and circular dichroism experiments to be associated with drug intercalation between base pairs. |
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Keywords: | Indoloquinoline DNA binding Cytotoxicity Spectroscopy |
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