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

IF 2.5 4区医学 Q3 CHEMISTRY, MEDICINAL

Bioorganic & Medicinal Chemistry Letters Pub Date : 2024-07-21 DOI:10.1016/j.bmcl.2024.129894

Mélanie Fonte , Catarina Rôla , Sofia Santana , Miguel Prudêncio , Joana Almeida , Ricardo Ferraz , Cristina Prudêncio , Cátia Teixeira , Paula Gomes

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Abstract

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.

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将抗疟药物重新用于癌症：探索 N-肉桂酰氨基吖啶的抗增殖作用。

作为扩大化疗药物组合的具有成本效益的方法，药物再利用和抢救已被广泛探讨。根据反式肉桂酸和抗疟氨基吖啶喹吖啶抗肿瘤特性的报道，我们探索了最近被确定为多级抗疟线索的两个系列 N-肉桂酰氨基吖啶的抗增殖特性。这些化合物针对三种癌细胞株（MKN-28、Huh-7 和 HepG2）和人类原发性真皮成纤维细胞进行了体外评估。其中一个系列的化合物在微摩尔范围内对所测试的三种癌细胞株显示出高度选择性的抗增殖活性，而对非致癌细胞没有任何毒性。

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来源期刊

Bioorganic & Medicinal Chemistry Letters 医学-医药化学

CiteScore

5.70

自引率

3.70%

发文量

463

审稿时长

27 days

期刊介绍： Bioorganic & Medicinal Chemistry Letters presents preliminary experimental or theoretical research results of outstanding significance and timeliness on all aspects of science at the interface of chemistry and biology and on major advances in drug design and development. The journal publishes articles in the form of communications reporting experimental or theoretical results of special interest, and strives to provide maximum dissemination to a large, international audience.