: Aurones are structural isomers of flavones and flavonols with the basic C6–C3–C6 skeleton arranged as (Z)-2-benzylidenebenzofuran-3(2H)-one, which contain an exocyclic carbon-carbon double bond bridging the benzofuranone and phenyl rings. In aurone, a chalcone-like group is closed into a 5-membered ring instead of the 6-membered ring more typical of flavonoids, which forms the core for a family of derivatives that are known collectively as aurones. As a kind of flavonoids, aurones are widely distributed in many plants which provide yellow color to some popular ornamental flowers. For a long time aurones had not got enough attention, while in recent years, finally this chemical is coming into researchers' view. As the secondary metabolite in the family of flavonoids, aurones displayed various biological activities, including antioxidant, antiparasitic, antitumor, antiviral, antibacterial, anti-inflammatory, anti-SARS-CoV-2 and neuropharmacological activities. Therefore, aurones have attracted the attention of more and more chemists and pharmaceutical chemists, who realized that it is possible to get lead compounds with better activities via structural modifications of aurones. In some research works, aurone and its derivatives have exhibited good activity, e.g., Xie discovered the heterocyclic variant of the (Z)-2-benzylidene-6-hydroxybenzofuran-3(2H)- one scaffold that possessed low nanomolar in vitro potency in cell proliferation assays using various cancer cell lines, in vivo potency in prostate cancer PC-3 xenograft and zebrafish models, and absence of appreciable toxicity, which proved that aurones are valuable compounds worthy of further study. Herein, the biological activities of aurone derivatives are reviewed, which covers the literature since 2000, in which the strategies to develop bioactive aurone derivatives and the structureactivity relationship are highlighted.

中文翻译：

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Aurones 的生物活性：简要总结

：Aurones 是黄酮和黄酮醇的结构异构体，其基本 C6-C3-C6 骨架排列为 (Z)-2-亚苄基苯并呋喃-3(2H)-one，其中包含桥接苯并呋喃酮和苯环的环外碳-碳双键。在金酮中，类似查耳酮的基团闭合成一个 5 元环，而不是更典型的黄酮类化合物的 6 元环，后者形成统称为金酮的衍生物家族的核心。作为一种黄酮类化合物，橙酮广泛分布于许多植物中，为一些流行的观赏花卉提供黄色。长期以来，Aurones并没有得到足够的重视，而近年来，这种化学物质终于进入了研究人员的视野。作为类黄酮家族的次级代谢产物，橙酮表现出多种生物活性，包括抗氧化、抗寄生虫、抗肿瘤、抗病毒、抗菌、抗炎、抗 SARS-CoV-2 和神经药理活性。因此，橙酮引起了越来越多的化学家和药物化学家的关注，他们意识到通过对橙酮的结构修饰可以获得具有更好活性的先导化合物。在一些研究工作中，Aurone及其衍生物表现出了良好的活性，例如Xie发现了(Z)-2-亚苄基-6-羟基苯并呋喃-3(2H)的杂环变体-一种在体外具有低纳摩尔效力的支架。使用各种癌细胞系进行的细胞增殖测定，在前列腺癌 PC-3 异种移植物和斑马鱼模型中的体内效力，并且没有明显的毒性，这证明了Aurones是值得进一步研究的有价值的化合物。本文对橙酮衍生物的生物活性进行了综述，涵盖了2000年以来的文献，其中重点介绍了生物活性橙酮衍生物的开发策略和构效关系。