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当代肿瘤药物靶点

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ISSN (Print): 1568-0096
ISSN (Online): 1873-5576

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Research Article

苯并三唑取代2-苯喹唑啉类抗癌药的合成、筛选、抗增殖及微管蛋白聚合抑制活性

卷 23, 期 4, 2023

发表于: 24 November, 2022

页: [278 - 292] 页: 15

弟呕挨: 10.2174/1568009623666221028121906

价格: $65

摘要

目的：微管蛋白靶向抗癌药物的研究进展。 背景：微管蛋白作为抗癌药物开发的重要靶点正在被探索。与小管蛋白秋水仙碱结合位点结合的配体作为小管蛋白聚合抑制剂，将细胞周期阻滞在G2/M期。 目的：苯并三唑取代2-苯基喹唑啉类抗癌药物的合成与筛选。 方法：一系列苯并三唑取代的喹唑啉衍生物已经被合成，并使用标准的MTT试验对人类MCF-7(乳腺癌)、HeLa(宫颈癌)和HT-29(结肠癌)癌细胞系进行了评估。 结果：ARV-2对MCF-7、HELA和HT29细胞的IC50分别为3.16 μM、5.31 μM和10.6 μM，表现出最强的抗增殖活性，而对正常细胞HEK293均无毒性。在细胞周期分析、凋亡实验和JC-1研究的机制研究中，发现ARV-2和ARV-3诱导线粒体介导的凋亡。 结论：苯并三唑取代的2-苯基喹唑啉类药物具有开发成有效抗癌药物的潜力。

关键词: 2-苯喹唑啉类，抗癌，抗增殖，微管蛋白聚合抑制剂，细胞周期，HeLa细胞。

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