摘要：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.
关键词：chloroquine;hydroxychloroquine;urea;antitumor activity in vitro
