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Carbocyclic potential DNA minor groove binders and their biological evaluation.
Drozdowska, Danuta; Bruzgo, Irena; Midura-Nowaczek, Krystyna.
Afiliação
  • Drozdowska D; Department of Organic Chemistry, Medical University, Bialystok, Poland. danuta.drozdowska@umwb.edu.pl
J Enzyme Inhib Med Chem ; 25(5): 629-34, 2010 Oct.
Article em En | MEDLINE | ID: mdl-20429779
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.
Assuntos

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Benzamidas / DNA / Inibidores de Serina Proteinase / Inibidores da Topoisomerase I / Inibidores da Topoisomerase II / Compostos de Anilina Limite: Humans Idioma: En Revista: J Enzyme Inhib Med Chem Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2010 Tipo de documento: Article País de afiliação: Polônia

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Benzamidas / DNA / Inibidores de Serina Proteinase / Inibidores da Topoisomerase I / Inibidores da Topoisomerase II / Compostos de Anilina Limite: Humans Idioma: En Revista: J Enzyme Inhib Med Chem Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2010 Tipo de documento: Article País de afiliação: Polônia