title: The quinobenzoxazines: relationship between DNA binding and biological activity.
abstract: The quinobenzoxazine compounds, derived from antibacterial quinolones, is active in vitro and in vivo against murine and human tumors. In this contribution, we show that the relative DNA binding affinity of the quinobenzoxazine compounds correlates with their cytotoxicity, their ability to inhibit gyrase-DNA complex formation, and the decatenation of kinetoplast DNA by human topoisomerase II. DNA binding studies with the descarboxy-A-62176 analogue indicate that the beta-keto acid moiety of the quinobenzoxazine compounds plays an important role in their interaction with DNA.
authors.affiliation: Drug Dynamics Institute, College of Pharmacy, The University of Texas at Austin, 78172-1074, USA.
authors.forename: Y
authors.initials: Y
authors.lastname: Kwok
authors.forename: D
authors.initials: D
authors.lastname: Sun
authors.forename: J J
authors.initials: JJ
authors.lastname: Clement
authors.forename: L H
authors.initials: LH
authors.lastname: Hurley
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000378:metabolism* / Q000494:pharmacology*; D001483:Base Sequence; D004247:DNA / Q000378:metabolism*; D018983:DNA Footprinting; D006801:Humans; D051379:Mice; D008969:Molecular Sequence Data; D010078:Oxazines / Q000378:metabolism* / Q000494:pharmacology*; D014407:Tumor Cells, Cultured
chemical_list: D000970:Antineoplastic Agents; D010078:Oxazines; D004247:DNA