2. Academic Validation
  3. Recycling antimalarial leads for cancer: Antiproliferative properties of N-cinnamoyl chloroquine analogues

Recycling antimalarial leads for cancer: Antiproliferative properties of N-cinnamoyl chloroquine analogues

  • Bioorg Med Chem Lett. 2013 Dec 15;23(24):6769-72. doi: 10.1016/j.bmcl.2013.10.025.
Bianca C Pérez 1,  Iva Fernandes,  Nuno Mateus,  Cátia Teixeira,  Paula Gomes
Affiliations

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.
PMID: 24184076 DOI: 10.1016/j.bmcl.2013.10.025
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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