Naslov
Chloroquine urea derivatives: synthesis and antitumor activity in vitro

Autori
Pavić, Kristina ; Rajić, Zrinka ; Mlinarić, Zvonimir ; Uzelac, Lidija ; Kralj, Marijeta ; Zorc, Branka

Izvornik
Acta pharmaceutica (1330-0075) 68 (2018), 4; 471-483

Vrsta, podvrsta i kategorija rada
Radovi u časopisima, članak, znanstveni

Ključne riječi
Chloroquine ; Hydroxychloroquine ; Urea ; Antitumor activity in vitro

Sažetak
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.

Izvorni jezik
Engleski

Znanstvena područja
Kemija, Temeljne medicinske znanosti, Farmacija

POVEZANOST RADA