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色烯查耳酮:从医学角度对其研究进展的全面综述

Chromenochalcones: a comprehensive review on developments towards a medicinal perspective.

作者信息

Singh Rohit, Katrolia Archita, Pal Ved

机构信息

Department of Pharmaceutical Chemistry, College of Pharmacy, JSS University C-1/A, Sector-62 Noida Uttar Pradesh India

Department of Pharmaceutics, College of Pharmacy, JSS University C-1/A, Sector-62 Noida Uttar Pradesh India

出版信息

RSC Med Chem. 2025 Apr 21. doi: 10.1039/d5md00062a.

Abstract

Chalcones are indeed a versatile scaffold in medicinal chemistry. Their structure, featuring an α,β-unsaturated carbonyl group, makes them highly reactive and capable of interacting with various biological targets. This reactivity is a key reason why chalcones and their derivatives are of such interest in drug discovery. The continued exploration of chalcone derivatives in medicinal chemistry will likely yield new insights and therapeutic candidates, given their broad spectrum of biological activities and the flexibility in modifying their structures. As chalcone derivatives, pyranochalcones and chromanchalcones are members of a subclass of flavonoids that are widely distributed. Several scientific databases were investigated to compile articles that illustrated the biological functions of chromenochalcones and their derivatives. Preclinical research on chromenochalcones and their derivatives is well covered in this review, highlighting the compounds with enormous significance as antimalarial, anti-inflammatory, antileishmanial, cytotoxic, antibacterial, antifungal, and antioxidant agents. In addition, the article briefly discusses the synthetic pathways employed for the total synthesis of selected pyranochalcones, including mallaophilippens C and E, citrunobin, and lesperol. Consequently, this overview may help research and design novel, potent therapeutic medications based on previously developed methodologies. This review is intended to provide a thorough, authoritative, and critical assessment of the chromenochalcone template for the chemistry community.

摘要

查耳酮确实是药物化学中一种用途广泛的骨架。它们的结构具有α,β-不饱和羰基,使其具有高反应性,并能够与各种生物靶点相互作用。这种反应性是查耳酮及其衍生物在药物发现中如此受关注的关键原因。鉴于查耳酮衍生物具有广泛的生物活性以及结构修饰的灵活性,在药物化学中对其持续探索可能会产生新的见解和治疗候选物。作为查耳酮衍生物,吡喃查耳酮和色满查耳酮是广泛分布的黄酮类化合物子类的成员。研究了几个科学数据库以汇编阐述色满查耳酮及其衍生物生物学功能的文章。本综述充分涵盖了色满查耳酮及其衍生物的临床前研究,突出了作为抗疟、抗炎、抗利什曼原虫、细胞毒性、抗菌、抗真菌和抗氧化剂具有重大意义的化合物。此外,本文简要讨论了用于全合成选定吡喃查耳酮(包括菲律宾马兜铃C和E、柠檬诺宾和莱斯佩罗尔)的合成途径。因此,这一概述可能有助于基于先前开发的方法研究和设计新型、有效的治疗药物。本综述旨在为化学界提供对色满查耳酮模板的全面、权威和批判性评估。

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本文引用的文献

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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。
Top Curr Chem (Cham). 2024 Jun 27;382(3):22. doi: 10.1007/s41061-024-00468-7.
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Chagas disease.恰加斯病
Lancet. 2024 Jan 13;403(10422):203-218. doi: 10.1016/S0140-6736(23)01787-7. Epub 2023 Dec 7.
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Leishmania: an urgent need for new treatments.利什曼原虫:对新疗法的迫切需求。
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Anticancer Activity of Natural and Synthetic Chalcones.天然和合成查耳酮的抗癌活性。
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A Review of Leishmaniasis: Current Knowledge and Future Directions.利什曼病综述:当前认知与未来方向
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