2. Academic Validation
  3. Small molecule glycoconjugates with anticancer activity

Small molecule glycoconjugates with anticancer activity

  • Eur J Med Chem. 2016 Apr 13:112:130-144. doi: 10.1016/j.ejmech.2016.01.061.
Gabriela Pastuch-Gawołek 1,  Katarzyna Malarz 2,  Anna Mrozek-Wilczkiewicz 3,  Marta Musioł 1,  Maciej Serda 2,  Barbara Czaplinska 2,  Robert Musiol 4
Affiliations

Affiliations

  • 1 Silesian University of Technology, Faculty of Chemistry, Chair of Organic Chemistry, Bioorganic Chemistry and Biotechnology, Krzywoustego 4, 44-100 Gliwice, Poland.
  • 2 Institute of Chemistry, University of Silesia, 9 Szkolna Street, 40-006 Katowice, Poland.
  • 3 A. Chełkowski Institute of Physics, University of Silesia, Uniwersytecka 4, 40-007 Katowice, Poland; Silesian Center for Education and Interdisciplinary Research, University of Silesia, 75 Pułku Piechoty 1A, 41-500 Chorzów, Poland.
  • 4 Institute of Chemistry, University of Silesia, 9 Szkolna Street, 40-006 Katowice, Poland. Electronic address: robert.musiol@us.edu.pl.
PMID: 26890119 DOI: 10.1016/j.ejmech.2016.01.061
Abstract

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.

Keywords

Anticancer; Chelators; Glycoconjugates; Quinoline; Reactive oxygen species.

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