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

resumo

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. (C) 2013 Elsevier Ltd. All rights reserved.

palavras-chave

HALF-MUSTARD DERIVATIVES; PHENYL NITROGEN-MUSTARD; AGENTS; ACID; DRUG; DISTAMYCIN; EXPRESSION; INHIBITORS; GROWTH; CELLS

categoria

Pharmacology & Pharmacy; Chemistry

autores

Perez, BC; Fernandes, I; Mateus, N; Teixeira, C; Gomes, P

nossos autores

Grupos

agradecimentos

This work was funded by FEDER Funds through the COMPETE program (Ref. FCOMP-01-0124-FEDER-020963) and by Portuguese National Funds through FCT-Fundacao para a Ciencia e Tecnologia (Ref. PTDC/QUI-QUI/116864/2010). B.P., I.F. and C.T. thank FCT for doctoral grant SFRH/BD/86166/2012 and post-doctoral grants SFRH/BPD/86173/2012 and SFRH/BPD/62967/2009, respectively.

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