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二苯乙烯衍生物构效关系的药物化学视角

Medicinal chemistry perspective on the structure-activity relationship of stilbene derivatives.

作者信息

Sepehri Saghi, Khedmati Mina, Yousef-Nejad Faeze, Mahdavi Mohammad

机构信息

Pharmaceutical Sciences Research Center, Ardabil University of Medical Sciences Ardabil Iran

Department of Medicinal Chemistry, School of Pharmacy, Ardabil University of Medical Sciences Ardabil Iran.

出版信息

RSC Adv. 2024 Jun 20;14(28):19823-19879. doi: 10.1039/d4ra02867h. eCollection 2024 Jun 18.

Abstract

Stilbenes are a small family of polyphenolic secondary metabolites produced in a variety of closely related plant species. These compounds function as phytoalexins, aiding plant defense against phytopathogens and plants' adaptation to abiotic environmental factors. Structurally, some important phenolic compounds have a 14-carbon skeleton and usually have two isomeric forms, and . Stilbenes contain two benzene rings linked by a molecule of ethanol or ethylene. Some derivatives of natural (poly)phenolic stilbenes such as resveratrol, pterostilbene, and combretastatin A-4 have shown various biological activities, such as anti-microbial, anti-cancer, and anti-inflammatory properties as well as protection against heart disease, Alzheimer's disease, and diabetes. Among stilbenes, resveratrol is certainly the most popular and extensively studied for its health properties. In recent years, an increasing number of stilbene compounds have been investigated for their bioactivity. This review focuses on the assessment of synthetic stilbene derivatives in terms of their biological activities and structure-activity relationship. The goal of this study is to consider the structural changes and different substitutions on phenyl rings that can improve the desired medicinal effects of stilbene-based compounds beyond the usual standards and subsequently discover biological activities by identifying effective alternatives of the evaluated compounds.

摘要

芪类化合物是一类小分子多酚类次生代谢产物,在多种近缘植物物种中产生。这些化合物作为植保素发挥作用,有助于植物抵御植物病原体以及适应非生物环境因素。在结构上,一些重要的酚类化合物具有14碳骨架,通常有两种异构体形式,即 和 。芪类化合物含有两个由一分子乙醇或乙烯连接的苯环。天然(多)酚类芪的一些衍生物,如白藜芦醇、紫檀芪和康普瑞他汀A - 4,已显示出各种生物活性,如抗菌、抗癌和抗炎特性,以及对心脏病、阿尔茨海默病和糖尿病的预防作用。在芪类化合物中,白藜芦醇因其健康特性无疑是最受欢迎且研究最广泛的。近年来,越来越多的芪类化合物因其生物活性受到研究。本综述重点评估合成芪类衍生物的生物活性及其构效关系。本研究的目的是考虑苯环上的结构变化和不同取代基,这些变化能够使芪类化合物的预期药用效果超越通常标准,并通过识别所评估化合物的有效替代物来发现生物活性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/163f/11188052/f64bd3e00b70/d4ra02867h-f1.jpg

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