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Chloroquine Urea Derivatives: Synthesis and Antitumor Activity in Vitro

Authors
  • Rajić, Kristina Pavić Zrinka
  • Mlinarić, Zvonimir
  • Uzelac, Lidija
  • Kralj, Marijeta
  • Zorc, Branka
Type
Published Article
Journal
Acta Pharmaceutica
Publisher
Sciendo
Publication Date
Oct 03, 2018
Volume
68
Issue
4
Pages
471–483
Identifiers
DOI: 10.2478/acph-2018-0039
Source
De Gruyter
Keywords
License
Green

Abstract

In the current paper, we describe the design, synthesis and antiproliferative screening of novel chloroquine derivatives with a quinoline core linked to a hydroxy or halogen amine through a flexible aminobutyl chain and urea spacer. Synthetic pathway leading to chloroquine urea derivatives 4-10 includes two crucial steps: i) synthesis of chloroquine benzotriazolide 3 and ii) formation of urea derivatives through the reaction of compound 3 with the corresponding amine. Testing of antiproliferative activity against four human cancer cell lines revealed that chloroquine urea derivatives 9 and 10 with aromatic moieties show activity at micromolar concentrations. Therefore, these molecules represent interesting lead compounds that might provide an insight into the design of new anticancer agents.

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