title: In vitro anticancer activity and evaluation of DNA duplex binding affinity of phenyl-substituted indoloquinolines.
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.
authors.affiliation: Institute of Biochemistry, Ernst-Moritz-Arndt University of Greifswald, Felix-Hausdorff-Strasse 4, D-17487 Greifswald, Germany.
authors.forename: Fanny
authors.initials: F
authors.lastname: Riechert-Krause
authors.forename: Andrea
authors.initials: A
authors.lastname: Eick
authors.forename: Renate
authors.initials: R
authors.lastname: Grünert
authors.forename: Patrick J
authors.initials: PJ
authors.lastname: Bednarski
authors.forename: Klaus
authors.initials: K
authors.lastname: Weisz
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry* / Q000627:therapeutic use / Q000633:toxicity; D045744:Cell Line, Tumor; D002942:Circular Dichroism; D004247:DNA / Q000737:chemistry*; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D007211:Indoles / Q000737:chemistry; D007364:Intercalating Agents / Q000737:chemistry* / Q000627:therapeutic use / Q000633:toxicity; D009369:Neoplasms / Q000188:drug therapy; D011804:Quinolines / Q000737:chemistry* / Q000627:therapeutic use / Q000633:toxicity; D013050:Spectrometry, Fluorescence; D044366:Transition Temperature
chemical_list: D000970:Antineoplastic Agents; D007211:Indoles; D007364:Intercalating Agents; D011804:Quinolines; C030374:indole; D004247:DNA; C037219:quinoline