深入了解查耳酮衍生物的合成策略、SAR 研究和抗癌机理:药物化学视角。

Q3 Medicine
Dipanjan Karati, Dileep Kumar
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引用次数: 0

摘要

查耳酮衍生物因其温和的化学性质、简便的合成方法和良好的生物活性而一直吸引着药物化学家。由于具有多种生物作用,它们已在治疗和制药行业广为人知。由于反应的灵活性,这些复合物在人体生物系统中具有不同的特性和应用,包括抗菌、抗肿瘤、抗疟和其他用途。因此,查耳酮在恶性肿瘤研究中引发了广泛关注。癌症的特征是异常细胞不受控制地生长和扩散以及细胞行为异常。这些肿块会破坏周围的正常组织,攻击重要器官,导致广泛的疾病。癌症经常被用作病人即将死亡的警告信号。在药物化学时代,癌症不可避免地引起人们的关注,并成为民众日益沉重的负担。所有恶性肿瘤的病理生理学都是由调节细胞发育、分裂和死亡的错误基因引起的。各种遗传和环境变量结合在一起,导致编码重要细胞调控蛋白的基因发生突变,从而导致癌症进化过程中的众多变化。新一代抗癌药物不是直接针对 DNA 合成,而是针对促进或控制细胞周期的信号、生长因子及其受体、信号转导途径以及影响 DNA 修复和死亡的途径。由于在寻找抗癌药物的过程中,不同化学结构的查尔酮衍生物至关重要,因此药物猎手们将注意力集中在了这些衍生物上。查尔酮的抗癌作用可归因于分子变化,如药物外流蛋白活性、激活细胞凋亡、DNA 和线粒体损伤、抑制血管生成、抑制微管蛋白和抑制激酶。查尔酮还可用于诊断癌症。开发查尔酮同系物作为抗癌原药或主要化学品需要进行深入研究。本综述介绍了近年来天然和合成查耳酮的不同药理活性。此外,还广泛记录了结构与活性的联系和过程,为今后的设计和合成提供了重要帮助。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
An Insight into Synthetic Strategies, SAR Study and Anticancer Mechanism of Chalcone Derivatives: Medicinal Chemistry Perspective.

Chalcone derivatives continue to captivate medicinal chemists due to their modest chemistry, facile synthetic method, and promising biological activities. They have become wellknown in the therapeutic and pharmaceutical industries due to their diverse biological actions. These complexes offer different features and applications in a human biological system due to the flexibility of the reactions, including antimicrobial, antineoplastic, antimalarial, and other uses. As a result, chalcones have sparked much attention in malignancy research. Cancer is characterized by uncontrollably growing and spreading abnormal cells and aberrant cell behavior. These masses destroy surrounding normal tissue and can attack vital organs, leading to widespread disease. Cancer is frequently used as a warning sign for impending patient death. In the age of pharmaceutical chemistry, it is unavoidably a cause for concern and a growing weight on the populace. The pathophysiology of all malignancies is due to faulty genes that regulate the development, division, and death of cells. Various genetic and environmental variables combine to cause mutations in genes encoding essential cell-regulatory proteins, leading to the numerous alterations that characterize the evolution of cancers. Rather than directly targeting DNA synthesis, the new generation of anticancer medications target signals that promote or control the cell cycle, growth factors and their receptors, signal transduction pathways, and pathways impacting DNA repair and death. Drug hunters are focusing their attention on chalcone derivatives with varying chemical structures since they are essential in the search for anticancer drugs. Chalcone's anticancer action may be attributed to molecular changes such as drug efflux protein activities, activation of apoptosis, DNA and mitochondrial damage, inhibition of angiogenesis, tubulin inhibition, and kinase inhibition. Chalcones are used to diagnose cancer as well. The development of chalcone congeners as a prodrug or prime chemical to combat cancer necessitates a thorough investigation. This review gives an update on the different pharmacological activities of natural and synthesized chalcones in recent years. Furthermore, the structure- activity connections and processes are extensively documented, providing essential design and synthesis assistance in the future.

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来源期刊
Current Drug Research Reviews
Current Drug Research Reviews Medicine-Psychiatry and Mental Health
CiteScore
3.70
自引率
0.00%
发文量
38
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