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Orientador(es)
Resumo(s)
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.
Descrição
Palavras-chave
Antitumor Cancer Covalent bitherapy Hybrid Malaria Mepacrine Recycling Selectivity
Contexto Educativo
Citação
Fonte, M., Rôla, C., Santana, S., Prudêncio, M., Almeida, J., Ferraz, R., Prudêncio, C., Teixeira, C., & Gomes, P. (2024). Repurposing antiplasmodial leads for cancer: Exploring the antiproliferative effects of N-cinnamoyl-aminoacridines. Bioorganic & Medicinal Chemistry Letters, 111, 129894. https://doi.org/10.1016/j.bmcl.2024.129894
Editora
Elsevier