酰胺链查尔酮衍生物,一类具有多种生物效应的有前途的化合物

IF 4.6 3区 化学 Q2 CHEMISTRY, MULTIDISCIPLINARY
RSC Advances Pub Date : 2025-06-05 DOI:10.1039/D5RA00834D
Omar Alshazly, Gamal El-Din A. Abuo-Rahma, Mamdouh F. A. Mohamed and Mohamed Abdel-Aziz
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引用次数: 0

摘要

查尔酮连接的乙酰胺衍生物是一类具有广泛生物活性的独特化合物。综述了查尔酮的各种合成方法,重点介绍了它们的效率。这些衍生物显示出有效的抗增殖特性,作为关键靶点的抑制剂,如EGFR、拓扑异构酶I和II、ABCG2、caspase蛋白和组蛋白去乙酰化酶(HDAC),以及抑制微管蛋白聚合。阐明了与它们的抗癌活性相关的构效关系。除了它们的抗增殖作用外,这些化合物对多种细菌和真菌病原体显示出显著的抗菌活性。它们的抗病毒潜力也被强调,具有抑制关键病毒酶和途径的能力。查尔酮连接的乙酰胺衍生物的抗原生动物特性强调了它们对原生动物感染的有效性。此外,这些衍生物具有很强的抗炎和抗氧化活性,有助于它们的整体治疗潜力。通过探索这些不同的生物活性,这些化合物为开发克服各种医学挑战的新型治疗剂提供了重要的机会。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Amide linked chalcone derivatives, a promising class of compounds with versatile biological effects

Amide linked chalcone derivatives, a promising class of compounds with versatile biological effects

Chalcone-linked acetamide derivatives represent a unique class of compounds with a broad spectrum of biological activities. Various synthetic methods for chalcones are reviewed, emphasizing their efficiency. These derivatives exhibited potent antiproliferative properties, functioning as inhibitors of key targets such as EGFR, topoisomerase I and II, ABCG2, caspase proteins, and histone deacetylase (HDAC), as well as inhibiting tubulin polymerization. The structure–activity relationships (SAR) pertinent to their anticancer activity are elucidated. In addition to their antiproliferative effects, these compounds display significant antimicrobial activities against a variety of bacterial and fungal pathogens. Their antiviral potential is also highlighted, with capabilities to inhibit critical viral enzymes and pathways. The antiprotozoal properties of chalcone-linked acetamide derivatives underscore their efficacy against protozoan infections. Furthermore, these derivatives possess strong anti-inflammatory and antioxidant activities, contributing to their overall therapeutic potential. By exploring these diverse biological activities, these compounds present significant opportunities for the development of novel therapeutic agents overcoming various medical challenges.

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来源期刊
RSC Advances
RSC Advances chemical sciences-
CiteScore
7.50
自引率
2.60%
发文量
3116
审稿时长
1.6 months
期刊介绍: An international, peer-reviewed journal covering all of the chemical sciences, including multidisciplinary and emerging areas. RSC Advances is a gold open access journal allowing researchers free access to research articles, and offering an affordable open access publishing option for authors around the world.
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