4.7 Article

Small molecule glycoconjugates with anticancer activity

期刊

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 112, 期 -, 页码 130-144

出版社

ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2016.01.061

关键词

Quinoline; Glycoconjugates; Reactive oxygen species; Anticancer; Chelators

资金

  1. NCN [2013/09/B/NZ7/00423, 2014/13/D/NZ7/00322]

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Glycoconjugates are combinations of sugar moieties with organic compounds. Due to their biological resemblance, such structures often have properties that are desirable for drugs. In this study we designed and synthesised several glycoconjugates from small molecular quinolines and substituted gluco- and galactopyranosyl amines. Although the parent quinoline compounds were inactive in affordable concentrations, the glycoconjugates that were obtained appeared to be cytotoxic against cancer cells at the micromolar level. When combined with copper ions, their activity increased even further. Their mechanism of action is connected to the formation of reactive oxygen species and the intercalation of DNA. (C) 2016 Elsevier Masson SAS. All rights reserved.

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