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查尔酮骨架在药物化学中的意义。

Significance of Chalcone Scaffolds in Medicinal Chemistry.

机构信息

Laboratory of Developing Drug Candidates, Department of Pharmacy, Tripura University (A Central University), Suryamaninagar, Agartala, Tripura, 799022, India.

Department of Microbiology and Biotechnology, School of Natural Sciences, Techno India University Tripura, Maheshkhola, Anandanagar, Agartala, Tripura, 799004, India.

出版信息

Top Curr Chem (Cham). 2024 Jun 27;382(3):22. doi: 10.1007/s41061-024-00468-7.

DOI:10.1007/s41061-024-00468-7
PMID:38937401
Abstract

Chalcone is a simple naturally occurring α,β-unsaturated ketone with biological importance, which can also be easily synthesized in laboratories by reaction between two aromatic scaffolds. In plants, chalcones occur as polyphenolic compounds of different frameworks which are bioactive molecules that have been in traditional medicinal practice for many years. Chalcone-based lead molecules have been developed, possessing varied potentials such as antimicrobial, antiviral, anti-inflammatory, anticancer, anti-oxidant, antidiabetic, antihyperurecemic, and anti-ulcer effects. Chalcones contribute considerable fragments to give important heterocyclic molecules with therapeutic utilities targeting various diseases. These characteristic features have made chalcone a topic of interest among researchers and have attracted investigations into this widely applicable structure. This review highlights the extensive exploration carried out on the synthesis, biotransformations, chemical reactions, hybridization, and pharmacological potentials of chalcones, and aims to provide an extensive, thorough, and critical review of their importance, with emphasis on their properties, chemistry, and biomedical applications to boost future investigations into this potential scaffold in medicinal chemistry.

摘要

查耳酮是一种具有生物学重要性的简单天然存在的α,β-不饱和酮,也可以通过两个芳基支架之间的反应在实验室中轻松合成。在植物中,查耳酮作为不同骨架的多酚化合物存在,是具有生物活性的分子,多年来一直用于传统医学实践。已经开发出基于查耳酮的先导分子,具有多种潜力,如抗菌、抗病毒、抗炎、抗癌、抗氧化、抗糖尿病、抗高尿酸血症和抗溃疡作用。查耳酮贡献了重要的片段,生成具有治疗各种疾病的治疗用途的重要杂环分子。这些特征使查耳酮成为研究人员关注的话题,并吸引了对这种广泛应用结构的研究。本综述重点介绍了对查耳酮的合成、生物转化、化学反应、杂交和药理学潜力的广泛探索,旨在对其重要性进行广泛、深入和批判性的综述,重点介绍其性质、化学和生物医学应用,以促进未来在药物化学中对这种潜在支架的研究。

相似文献

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Significance of Chalcone Scaffolds in Medicinal Chemistry.查尔酮骨架在药物化学中的意义。
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引用本文的文献

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Pharmacological potential of natural chalcones: a recent studies and future perspective.天然查尔酮的药理潜力:近期研究与未来展望
Front Pharmacol. 2025 Jun 17;16:1570385. doi: 10.3389/fphar.2025.1570385. eCollection 2025.
2
Carboxychalcones Based on Terephthalaldehydic Acid as Potential Neuroprotective Agents. Synthesis, Computational Study and Biological Evaluation.基于对苯二甲醛的羧基查尔酮作为潜在神经保护剂的研究。合成、计算研究及生物学评价
ACS Omega. 2025 May 7;10(19):19860-19872. doi: 10.1021/acsomega.5c01417. eCollection 2025 May 20.
3
Chromenochalcones: a comprehensive review on developments towards a medicinal perspective.

本文引用的文献

1
Anticancer Potential of Natural Chalcones: In Vitro and In Vivo Evidence.天然查耳酮的抗癌潜力:体外和体内证据。
Int J Mol Sci. 2023 Jun 19;24(12):10354. doi: 10.3390/ijms241210354.
2
Evaluation of a preemptive intervention regimen with hesperidin methyl chalcone in delayed-onset muscle soreness in young adults: a randomized, double-blinded, and placebo-controlled trial study.评价橙皮苷甲查尔酮预先干预方案对年轻人迟发性肌肉酸痛的效果:一项随机、双盲、安慰剂对照试验研究。
Eur J Appl Physiol. 2023 Sep;123(9):1949-1964. doi: 10.1007/s00421-023-05207-2. Epub 2023 Apr 29.
3
Bis-chalcones: A review of synthetic methodologies and anti-inflammatory effects.
色烯查耳酮:从医学角度对其研究进展的全面综述
RSC Med Chem. 2025 Apr 21. doi: 10.1039/d5md00062a.
4
Radiolabeled Probes from Derivatives of Natural Compounds Used in Nuclear Medicine.放射性标记探针来源于核医学中天然化合物的衍生物。
Molecules. 2024 Sep 8;29(17):4260. doi: 10.3390/molecules29174260.
双查耳酮:合成方法学和抗炎作用综述。
Eur J Med Chem. 2023 Apr 5;252:115280. doi: 10.1016/j.ejmech.2023.115280. Epub 2023 Mar 16.
4
Hesperidin methyl chalcone, a citrus flavonoid, inhibits Aeromonas hydrophila infection mediated by quorum sensing.橙皮苷甲基查耳酮,一种柑橘类黄酮,可抑制群体感应介导的嗜水气单胞菌感染。
Microb Pathog. 2023 Apr;177:106029. doi: 10.1016/j.micpath.2023.106029. Epub 2023 Feb 10.
5
Chalcones: Promising therapeutic agents targeting key players and signaling pathways regulating the hallmarks of cancer.查耳酮:靶向调控癌症特征的关键因子和信号通路的有前景的治疗药物。
Chem Biol Interact. 2023 Jan 5;369:110297. doi: 10.1016/j.cbi.2022.110297. Epub 2022 Dec 7.
6
Novel quorum sensing inhibitor Echinatin as an antibacterial synergist against .新型群体感应抑制剂松脂素作为针对……的抗菌增效剂
Front Microbiol. 2022 Nov 1;13:1003692. doi: 10.3389/fmicb.2022.1003692. eCollection 2022.
7
Chalcone: A Promising Bioactive Scaffold in Medicinal Chemistry.查尔酮:药物化学中一种有前景的生物活性骨架。
Pharmaceuticals (Basel). 2022 Oct 11;15(10):1250. doi: 10.3390/ph15101250.
8
Dipeptidyl peptidase-4 inhibitory potentials of and its bioactive compounds licochalcone A and licochalcone B: An and study.及其生物活性化合物甘草查尔酮A和甘草查尔酮B的二肽基肽酶-4抑制潜力:一项[具体研究类型]和[具体研究类型]研究。 (注:原文中“and”重复使用,推测可能是有具体的研究类型未完整给出,这里只能按原样翻译)
Front Mol Biosci. 2022 Sep 30;9:1024764. doi: 10.3389/fmolb.2022.1024764. eCollection 2022.
9
Structural modification and antibacterial property studies of natural chalcone sanjuanolide.天然查耳酮桑乔内酯的结构修饰与抗菌性能研究
Front Chem. 2022 Aug 5;10:959250. doi: 10.3389/fchem.2022.959250. eCollection 2022.
10
Synthesis of Chalcones Derivatives and Their Biological Activities: A Review.查尔酮衍生物的合成及其生物活性:综述
ACS Omega. 2022 Aug 2;7(32):27769-27786. doi: 10.1021/acsomega.2c01779. eCollection 2022 Aug 16.