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

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:23

Article

Perez, Bianca C.¹  Fernandes, Iva¹  Mateus, Nuno¹  Teixeira, Catia^1,2  Gomes, Paula¹ 

[1] Univ Porto, Ctr Invest Quim, Dept Quim Bioquim, Fac Ciencias, P-4169007 Oporto, Portugal

[2] Univ Aveiro, Dept Quim, CICECO, P-3810193 Aveiro, Portugal

关键词: Antimalarials;    Antiproliferative;    Caco-2;    Chloroquine;    Cinnamic acid;    HFF-1;    MCF-7;    MKN-28;   

DOI  :  10.1016/j.bmcl.2013.10.025

来源: Elsevier

【 摘 要 】

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.

【 授权许可】

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