Abstract

A series of imines 5-amino-1,3,4-thiadiazol-2-[(N-substituted benzyol)]sulphonamide derivatives were synthesized from various aromatic aldehydes and substituted with benzoyl acetazolamides under different reaction conditions and were evaluated for their antioxidant and free radical scavenging, antimitotic activity by Allium cepa meristem root model and cytotoxicity activity against HEK 293 (human epidermal kidney cell line), BT474 (breast cancer cell line) and NCI-H226 (lung cancer cell line) by MTT assay. Some of the synthesized compounds showed moderately potent cytotoxicity compared to indisulam.

Graphical abstract

A series of imines 5-amino-1,3,4-thiadiazol-2-[(N-substituted benzyol)]sulphonamide derivatives (9a–j); 5-amino-1,3,4-thiadiazol-2-[N-(substituted benzoyl)]sulphonamide (4a–g); 5-(4-acetamido phenyl sulphonamido)-1,3,4-thiadiazol-2-[N-(substituted benzoyl)]sulphonamide (6a–g); and 5-(4-amino phenyl sulphonamido)-1,3,4-thiadiazol-2-[N-(substituted benzoyl)]sulphonamide (7a–g) were synthesized from acetazolamide and were investigated for the in vitro anticancer by MTT assay, free radical scavenging and antimitotic activity by Allium cepa root meristem model. Experimental observations indicate that synthesized compounds were moderately potent anticancer agents.

中文翻译：

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5-芳基氨基-1,3,4-噻二唑-2-[(N-取代苄醇)]磺酰胺的合成具有有效的抗氧化剂和抗癌活性，可诱导 HEK293、BT474 和 NCI-H226 细胞的生长抑制。

摘要

以各种芳香醛为原料合成了一系列亚胺5-氨基-1,3,4-噻二唑-2-[( N-取代苄醇)]磺酰胺衍生物，并在不同反应条件下被苯甲酰乙酰唑酰胺取代，并评价了它们的抗氧化性和抗氧化性。自由基清除、洋葱分生组织根模型的抗有丝分裂活性以及 MTT 测定对 HEK 293（人表皮肾细胞系）、BT474（乳腺癌细胞系）和 NCI-H226（肺癌细胞系）的细胞毒性活性。一些合成的化合物与吲哚美林相比显示出中等强度的细胞毒性。

图形概要

一系列亚胺 5-氨基-1,3,4-噻二唑-2-[( N-取代苄醇)]磺酰胺衍生物 ( 9a – j ); 5-氨基-1,3,4-噻二唑-2-[ N- (取代苯甲酰基)]磺酰胺( 4a - g )；5-(4-乙酰氨基苯基磺酰胺)-1,3,4-噻二唑-2-[ N- (取代苯甲酰基)]磺酰胺( 6a - g )；和 5-(4-amino phenyl sulfonamido)-1,3,4-thiadiazol-2-[ N- (取代苯甲酰基)]sulphonamide ( 7a – g ) 是从乙酰唑胺合成的，并通过 MTT 法研究了体外抗癌作用, 自由基清除和抗有丝分裂活性洋葱根分生组织模型。实验观察表明合成的化合物是中等有效的抗癌剂。