Abstract

Herein, we synthesized some new indole-1,3,4-oxadiazole based sulfonyl 1,2,3-triazoles via a click chemistry approach and then characterized their structures by NMR, mass, and CHN analysis techniques. Later, the anticancer activity of the synthesized compounds was screened in vitro against different human cancer cell lines like MCF-7 and A-549, and the results were compared with the standard drug erlotinib. Most of the investigated compounds were found to be active against both cancer cell lines, MCF-7, and A-459. Specifically, compounds 2-(((1-(4-chloro-3,5-dimethoxyphenyl)-1H-1,2,3-triazol-4-yl)methyl)sulfonyl)-5-(1-methyl-1H-indol-3-yl)-1,3,4-oxadiazole and 2-(((1-(3,5-dichlorophenyl)-1H-1,2,3-triazol-4-yl)methyl) sulfonyl)-5-(1-methyl-1H-indol-3-yl)-1,3,4-oxadiazole had superior activity against MCF-7, and remarkable activity against A-549. Similarly, the compound 2-(((1-(3,5-dichlorophenyl)-1H-1,2,3-triazol-4-yl)methyl)sulfonyl)-5-(1-methyl-1H-indol-3-yl)-1,3,4-oxadiazole showed more potent activity against EGFR and compound 2-(((1-(4-chloro-3,5-dimethoxyphenyl)-1H-1,2,3-triazol-4-yl)methyl)sulfonyl)-5-(1-methyl-1H-indol-3-yl)-1,3,4-oxadiazole showed equipotent activity against tyrosine kinase EGFR inhibitory activity.

中文翻译：

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基于吲哚-1,3,4-恶二唑的磺酰基 1,2,3-三唑的合成作为有效抗癌和 EGFR 抑制剂

摘要

在此，我们通过点击化学方法合成了一些新的吲哚-1,3,4-恶二唑基磺酰基1,2,3-三唑，然后通过核磁共振、质量和CHN分析技术表征了它们的结构。随后，在体外筛选了合成化合物针对MCF-7和A-549等不同人类癌细胞系的抗癌活性，并将结果与​​标准药物厄洛替尼进行了比较。大多数研究的化合物被发现对两种癌细胞系 MCF-7 和 A-459 都有活性。具体地，化合物2-(((1-(4-氯-3,5-二甲氧基苯基)-1H-1,2,3-三唑-4-基)甲基)磺酰基)-5-(1-甲基-1H-吲哚-3-基)-1,3,4-恶二唑和2-(((1-(3,5-二氯苯基)-1H-1,2,3-三唑-4-基)甲基)磺酰基)-5 -(1-甲基-1H-吲哚-3-基)-1,3,4-恶二唑对MCF-7具有优异的活性，对A-549具有显着的活性。类似地，化合物2-(((1-(3,5-二氯苯基)-1H-1,2,3-三唑-4-基)甲基)磺酰基)-5-(1-甲基-1H-吲哚-3 -基)-1,3,4-恶二唑对 EGFR 和化合物 2-(((1-(4-氯-3,5-二甲氧基苯基)-1H-1,2,3-三唑-4-基)甲基)磺酰基)-5-(1-甲基-1H-吲哚-3-基)-1,3,4-恶二唑对酪氨酸激酶 EGFR 抑制活性具有同等活性。