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Review Article

噻唑及其相关杂环系统作为抗癌药物的合成策略、作用机制和SAR研究综述

卷 29, 期 29, 2022

发表于: 10 May, 2022

页: [4958 - 5009] 页: 52

弟呕挨: 10.2174/0929867329666220318100019

价格: $65

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摘要

背景：癌症是全球第二大死亡原因。许多抗癌药物已经上市，但缺乏选择性、靶点特异性、细胞毒性和耐药性的发展会导致严重的副作用。已经进行了一些实验来开发副作用小或没有副作用的化合物。 目的：综述噻唑、苯并噻唑、咪唑噻唑化合物作为抗癌药物的合成策略、SAR研究及其作用机制。 方法：综述了近年来有关噻唑和噻唑相关衍生物的抗癌潜力的文献。本文综述了当代噻唑及其相关衍生物的合成策略、机理靶点和全面的结构活性关系研究，为合理设计高效噻唑类抗癌候选药物提供了展望。 结果：详尽的文献调查表明，噻唑衍生物与诱导细胞凋亡和干扰微管蛋白组装的特性有关。噻唑还与NFkB/mTOR/PI3K/AkT的抑制和雌激素介导的活性的调节有关。此外，噻唑衍生物已被发现可以调节关键靶点，如拓扑异构酶和HDAC。 结论：噻唑衍生物具有良好的活性，并通过多种机制发挥作用。部分噻唑衍生物，如化合物29、40、62和74a，半抑制浓度值分别为0.05 μM、0.00042 μM、0.18 μM和0.67 μM，不仅具有抗癌活性，而且具有较低的毒性和较好的吸收能力。因此，还可以研究其他一些类似的化合物来帮助开发抗癌药效团。

关键词: 噻唑类，抗癌，合成，靶标，SAR，分子对接，耐药性，杂环系统。

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