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Recycling antimalarial leads for cancer: Antiproliferative properties of N-cinnamoyl chloroquine analogues
Authors:Bianca C. Pérez  Iva Fernandes  Nuno Mateus  Cátia Teixeira  Paula Gomes
Affiliation:1. Centro de Investigação em Química da Universidade do Porto, Departamento de Química e Bioquímica, Faculdade de Ciências, Universidade do Porto, Rua do Campo Alegre 687, P-4169-007 Porto, Portugal;2. CICECO, Departamento de Química, Universidade de Aveiro, Campus Universitário de Santiago, 3810-193 Aveiro, Portugal
Abstract:Cinnamic acids and quinolines are known as useful scaffolds in the discovery of antitumor agents. Therefore, N-cinnamoylated analogues of chloroquine, recently reported as potent dual-action antimalarials, were evaluated against three different cancer cell lines: MKN-28, Caco-2, and MCF-7. All compounds display anti-proliferative activity in the micromolar range against the three cell lines tested, and most of them were more active than their parent drug, chloroquine, against all cell lines tested. Hence, N-cinnamoyl-chloroquine analogues are a good start towards development of affordable antitumor leads.
Keywords:Antimalarials  Antiproliferative  Caco-2  Chloroquine  Cinnamic acid  HFF-1  MCF-7  MKN-28
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