<abstract xmlns="http://www.w3.org/1999/xhtml"><p> 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.</p></abstract>

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.

Chloroquine Urea Derivatives: Synthesis and Antitumor Activity in Vitro

Acta Pharmaceutica

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 License.

{"article-title":"Chloroquine Urea Derivatives: Synthesis and Antitumor Activity in Vitro"}

In the current paper, we describe the design, synthesis and antiproliferative screening of novel chloroquine derivatives with a quinoline core linked to a...

Chloroquine Urea Derivatives: Synthesis and Antitumor Activity in Vitro

Published Online: Oct 03, 2018

Page range: 471 - 483

Received: Sep 11, 2018

Accepted: Sep 14, 2018

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

Keywords
chloroquine, hydroxychloroquine, urea, antitumor activity in vitro

© 2018 Kristina Pavić Zrinka Rajić, published by Sciendo

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 License.

Chloroquine Urea Derivatives: Synthesis and Antitumor Activity in Vitro

Published Online: Oct 03, 2018

Page range: 471 - 483

Received: Sep 11, 2018

Accepted: Sep 14, 2018

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

Keywordschloroquine, hydroxychloroquine, urea, antitumor activity in vitro

© 2018 Kristina Pavić Zrinka Rajić, published by Sciendo

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 License.

Keywords
chloroquine, hydroxychloroquine, urea, antitumor activity in vitro