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https://doi.org/10.2478/acph-2018-0039

Chloroquine urea derivatives: synthesis and antitumor activity in vitro

KRISTINA PAVIĆ ; University of Zagreb Faculty of Pharmacy and Biochemistry, Department of Medicinal Chemistry, HR-10 000 Zagreb, Croatia
ZRINKA RAJIĆ ; University of Zagreb Faculty of Pharmacy and Biochemistry, Department of Medicinal Chemistry, HR-10 000 Zagreb, Croatia
ZVONIMIR MLINARIĆ orcid id orcid.org/0000-0003-2571-2461 ; University of Zagreb Faculty of Pharmacy and Biochemistry, Department of Medicinal Chemistry, HR-10 000 Zagreb, Croatia
LIDIJA UZELAC orcid id orcid.org/0000-0002-3076-7064 ; Rudjer Bošković Institute, Division of Molecular Medicine, Laboratory of Experimental Therapy, HR-10 000 Zagreb, Croatia
MARIJETA KRALJ ; Rudjer Bošković Institute, Division of Molecular Medicine, Laboratory of Experimental Therapy, HR-10 000 Zagreb, Croatia
BRANKA ZORC orcid id orcid.org/0000-0003-4355-8816 ; University of Zagreb Faculty of Pharmacy and Biochemistry, Department of Medicinal Chemistry, HR-10 000 Zagreb, Croatia


Puni tekst: engleski pdf 413 Kb

str. 471-483

preuzimanja: 304

citiraj


Sažetak

In the current paper, we describe 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 the 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 in micromolar concentrations. Therefore, these molecules represent interesting lead compounds that might provide insight into the design of new anticancer agents.

Ključne riječi

chloroquine, hydroxychloroquine, urea, antitumor activity in vitro

Hrčak ID:

203273

URI

https://hrcak.srce.hr/203273

Posjeta: 954 *