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近年来喹啉类化合物在抗疟和抗癌药物研发中的贡献。

Recent contributions of quinolines to antimalarial and anticancer drug discovery research.

机构信息

SynBioC Research Group, Department of Green Chemistry and Technology, Faculty of Bioscience Engineering, Ghent University, Coupure Links 653, B-9000, Ghent, Belgium.

SynBioC Research Group, Department of Green Chemistry and Technology, Faculty of Bioscience Engineering, Ghent University, Coupure Links 653, B-9000, Ghent, Belgium.

出版信息

Eur J Med Chem. 2021 Dec 15;226:113865. doi: 10.1016/j.ejmech.2021.113865. Epub 2021 Sep 23.

Abstract

Quinoline, a privileged scaffold in medicinal chemistry, has always been associated with a multitude of biological activities. Especially in antimalarial and anticancer research, quinoline played (and still plays) a central role, giving rise to the development of an array of quinoline-containing pharmaceuticals in these therapeutic areas. However, both diseases still affect millions of people every year, pointing to the necessity of new therapies. Quinolines have a long-standing history as antimalarial agents, but established quinoline-containing antimalarial drugs are now facing widespread resistance of the Plasmodium parasite. Nevertheless, as evidenced by a massive number of recent literature contributions, they are still of great value for future developments in this field. On the other hand, the number of currently approved anticancer drugs containing a quinoline scaffold are limited, but a strong increase and interest in quinoline compounds as potential anticancer agents can be seen in the last few years. In this review, a literature overview of recent contributions made by quinoline-containing compounds as potent antimalarial or anticancer agents is provided, covering publications between 2018 and 2020.

摘要

喹啉作为药物化学中的一个重要结构骨架,一直与多种生物活性相关联。特别是在抗疟和抗癌研究中,喹啉发挥了(并且仍然发挥着)核心作用,在这些治疗领域产生了一系列含喹啉的药物。然而,这两种疾病每年仍影响着数以百万计的人,这表明需要新的治疗方法。喹啉作为抗疟药物已有很长的历史,但目前已有的含喹啉的抗疟药物正面临疟原虫广泛耐药的问题。尽管如此,大量最近的文献研究表明,它们在该领域的未来发展中仍然具有重要价值。另一方面,目前批准的含有喹啉结构的抗癌药物数量有限,但近年来,喹啉化合物作为潜在抗癌药物的潜力引起了人们的强烈关注和兴趣。在这篇综述中,提供了 2018 年至 2020 年期间有关含喹啉化合物作为有效抗疟或抗癌剂的最新文献综述。

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