Chloroquine Urea Derivatives: Synthesis and Antitumor Activity in Vitro

Clics: 256
ID: 107742
2018
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Ranked #24 of 56 articles by views in acta pharmaceutica

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Resumen
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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Autores Kristina, Pavić;Zrinka, Rajić;Zvonimir, Mlinarić;Lidija, Uzelac;Marijeta, Kralj;Branka, Zorc;
Revista acta pharmaceutica
Ano 2018
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