Repurposing antiplasmodial leads for cancer: Exploring the antiproliferative effects of N-cinnamoyl-aminoacridines

• Type: Article in International Scientific Journal
• Date: 2024

Authors

Fonte, M (Author) Other; Rôla, C (Author) Other; Santana, S (Author) Other; Prudêncio, M (Author) Other; Almeida, J (Author) Other; Ferraz, R (Author) Other; Prudêncio, C (Author) Other; Teixeira, C (Author) Other; Paula Gomes (Author) FCUP

Journal

Title: Bioorganic and Medicinal Chemistry Letters

Vol. 111

ISSN: 0960-894X

Publisher: Elsevier

Indexing

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Other information

Authenticus ID: P-012-MNT

DOI: 10.1016/j.bmcl.2024.129894

Abstract (EN): 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.

Language: English

Type (Professor's evaluation): Scientific

No. of pages: 4