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综述:探究单羰基姜黄素类似物的合成方案及构效关系(SAR)研究对细胞毒性抑制抗癌活性的影响。

A Review: Exploring Synthetic Schemes and Structure-activity Relationship (SAR) Studies of Mono-carbonyl Curcumin Analogues for Cytotoxicity Inhibitory Anticancer Activity.

机构信息

Department of Pharmaceutical Chemistry, A.I.S.S.M.S College of Pharmacy, Near RTO, Kennedy Road, Pune, 411001, Maharashtra, India.

Department of Chemical Technology, Dr. Babasaheb Ambedkar Marathwada University, Aurangabad, 431004, Maharashtra, India.

出版信息

Curr Org Synth. 2023;20(8):821-837. doi: 10.2174/1570179420666230126142238.

Abstract

INTRODUCTION

Cancer is the major cause of death globally. Cancer can be treated with naturally occurring Curcumin nuclei. Curcumin has a wide range of biological actions, including anti-inflammatory and anti-cancer properties. Even though it is an effective medicinal entity, it has some limitations such as instability at physiological pH and a weak pharmacokinetic profile due to the β-diketone moiety present in it. To overcome this drawback, research was carried out on monoketone moieties in curcumin, popularly known as mono-carbonyl curcumin.

OBJECTIVE

The present review focuses on different synthetic schemes and Mono-carbonyl curcumin derivative's Structure-Activity Relationship (SAR) as a cytotoxic inhibitory anticancer agent. The various synthetic schemes published by researchers were compiled.

METHODS

Findings of different researchers working on mono-carbonyl curcumin as an anticancer have been reviewed, analyzed and the outcomes were summarized.

RESULTS

The combination of all of these approaches serves as a one-stop solution for mono-carbonyl curcumin synthesis. The important groups on different positions of mono-carbonyl curcumin were discovered by a SAR study focused on cytotoxicity, which could be useful in the designing of its derivatives.

CONCLUSION

Based on our examination of the literature, we believe that this review will help researchers design and develop powerful mono-carbonyl curcumin derivatives that can be proven essential for anticancer activity.

摘要

简介

癌症是全球主要的死亡原因。癌症可以用天然存在的姜黄素核治疗。姜黄素具有广泛的生物学作用,包括抗炎和抗癌特性。尽管它是一种有效的药物实体,但由于其存在的β-二酮部分,它在生理 pH 值下不稳定且药代动力学特征较弱,因此存在一些限制。为了克服这一缺点,对姜黄素中的单酮部分进行了研究,通常称为单羰基姜黄素。

目的

本综述重点介绍了不同的合成方案和单羰基姜黄素衍生物的构效关系(SAR)作为细胞毒性抑制抗癌剂。编译了研究人员发表的各种合成方案。

方法

综述了不同研究人员在单羰基姜黄素作为抗癌药物方面的研究结果,对其进行了分析和总结。

结果

通过对细胞毒性的 SAR 研究,发现了单羰基姜黄素不同位置上的重要基团,这可能有助于设计其衍生物。

结论

根据我们对文献的研究,我们相信这篇综述将有助于研究人员设计和开发具有强大抗癌活性的单羰基姜黄素衍生物。

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