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Original scientific paper
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 icon 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 icon 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 icon orcid.org/0000-0003-4355-8816 ; University of Zagreb Faculty of Pharmacy and Biochemistry, Department of Medicinal Chemistry, HR-10 000 Zagreb, Croatia

Fulltext: english, pdf (413 KB) pages 471-483 downloads: 102* cite
APA 6th Edition
PAVIĆ, K., RAJIĆ, Z., MLINARIĆ, Z., UZELAC, L., KRALJ, M. & ZORC, B. (2018). Chloroquine urea derivatives: synthesis and antitumor activity in vitro. Acta Pharmaceutica, 68 (4), 471-483. https://doi.org/10.2478/acph-2018-0039
MLA 8th Edition
PAVIĆ, KRISTINA, et al. "Chloroquine urea derivatives: synthesis and antitumor activity in vitro." Acta Pharmaceutica, vol. 68, no. 4, 2018, pp. 471-483. https://doi.org/10.2478/acph-2018-0039. Accessed 26 Jan. 2020.
Chicago 17th Edition
PAVIĆ, KRISTINA, ZRINKA RAJIĆ, ZVONIMIR MLINARIĆ, LIDIJA UZELAC, MARIJETA KRALJ and BRANKA ZORC. "Chloroquine urea derivatives: synthesis and antitumor activity in vitro." Acta Pharmaceutica 68, no. 4 (2018): 471-483. https://doi.org/10.2478/acph-2018-0039
Harvard
PAVIĆ, K., et al. (2018). 'Chloroquine urea derivatives: synthesis and antitumor activity in vitro', Acta Pharmaceutica, 68(4), pp. 471-483. https://doi.org/10.2478/acph-2018-0039
Vancouver
PAVIĆ K, RAJIĆ Z, MLINARIĆ Z, UZELAC L, KRALJ M, ZORC B. Chloroquine urea derivatives: synthesis and antitumor activity in vitro. Acta Pharm. [Internet]. 2018 [cited 2020 January 26];68(4):471-483. https://doi.org/10.2478/acph-2018-0039
IEEE
K. PAVIĆ, Z. RAJIĆ, Z. MLINARIĆ, L. UZELAC, M. KRALJ and B. ZORC, "Chloroquine urea derivatives: synthesis and antitumor activity in vitro", Acta Pharmaceutica, vol.68, no. 4, pp. 471-483, 2018. [Online]. https://doi.org/10.2478/acph-2018-0039

Abstracts
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.

Keywords
chloroquine; hydroxychloroquine; urea; antitumor activity in vitro

Hrčak ID: 203273

URI
https://hrcak.srce.hr/203273

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