title: Carbocyclic potential DNA minor groove binders and their biological evaluation.
abstract: The biological evaluation of carbocyclic minor groove binders 1-6 is described. The cytotoxicity of the obtained compounds was tested on MDA-MB-231 breast cancer cells. The mechanism of action of compounds 1-6 was studied employing the topoisomerase I/II inhibition assay and ethidium displacement assay using pBR322. Determination of association constants was done using calf thymus DNA, T4 coliphage DNA, poly(dA-dT)(2), and poly(dG-dC)(2). The effect of compounds 1-6 on the amidolytic activity of plasmin, trypsin, thrombin, and urokinase was also examined.
authors.affiliation: Department of Organic Chemistry, Medical University, Białystok, Poland. danuta.drozdowska@umwb.edu.pl
authors.forename: Danuta
authors.initials: D
authors.lastname: Drozdowska
authors.forename: Irena
authors.initials: I
authors.lastname: Bruzgo
authors.forename: Krystyna
authors.initials: K
authors.lastname: Midura-Nowaczek
mesh_terms: D000814:Aniline Compounds / Q000378:metabolism* / Q000494:pharmacology*; D017122:Bacteriophage T4; D001549:Benzamides / Q000378:metabolism* / Q000494:pharmacology*; D001667:Binding, Competitive; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004247:DNA / Q000378:metabolism*; D004278:DNA, Superhelical / Q000378:metabolism; D004279:DNA, Viral / Q000378:metabolism; D015195:Drug Design; D004996:Ethidium / Q000378:metabolism; D006801:Humans; D020128:Inhibitory Concentration 50; D007700:Kinetics; D010957:Plasmids; D011089:Polydeoxyribonucleotides / Q000378:metabolism; D015842:Serine Proteinase Inhibitors / Q000378:metabolism* / Q000494:pharmacology*; D059004:Topoisomerase I Inhibitors / Q000378:metabolism* / Q000494:pharmacology*; D059005:Topoisomerase II Inhibitors / Q000378:metabolism* / Q000494:pharmacology*
chemical_list: D000814:Aniline Compounds; D001549:Benzamides; D004278:DNA, Superhelical; D004279:DNA, Viral; D011089:Polydeoxyribonucleotides; D015842:Serine Proteinase Inhibitors; D059004:Topoisomerase I Inhibitors; D059005:Topoisomerase II Inhibitors; D004247:DNA; C427203:calf thymus DNA; D004996:Ethidium