Author(s): Fonte, Mélanie ; Rôla, Catarina ; Santana, Sofia ; Ferraz, Ricardo ; Prudêncio, Miguel ; Almeida, Joana ; Ferraz, Ricardo ; Prudêncio, Cristina ; Teixeira, Cátia ; Gomes, Paula
Date: 2024
Persistent ID: http://hdl.handle.net/10400.22/26225
Origin: Repositório Científico do Instituto Politécnico do Porto
Subject(s): Antitumor; Cancer; Covalent bitherapy; Hybrid; Malaria; Mepacrine; Recycling; Selectivity
Drug repurposing and rescuing have been widely explored as cost-effective approaches to expand the portfolio of chemotherapeutic agents. Based on the reported antitumor properties of both trans-cinnamic acids and quinacrine, an antimalarial aminoacridine, we explored the antiproliferative properties of two series of N-cinnamoyl-aminoacridines recently identified as multi-stage antiplasmodial leads. The compounds were evaluated in vitro against three cancer cell lines (MKN-28, Huh-7, and HepG2), and human primary dermal fibroblasts. One of the series displayed highly selective antiproliferative activity in the micromolar range against the three cancer cell lines tested, without any toxicity to non-carcinogenic cells.
