Abstract

A series of novel thiadiazole-incorporated aminothiazole derivatives were synthesized and characterized by IR and ¹H NMR and ¹³C NMR spectroscopy, ESI mass spectrometry, and elemental analysis. All the synthesized compounds were tested for their in vitro anticancer activity against MCF-7, A549, and HeLa human cancer cell lines by the MTT assay. 5-(1-{2-[4-(4-Nitrophenyl)thiazol-2-yl]hydrazono}ethyl)-3-phenyl-1,3,4-thiadiazol-2(3H)-imine and 5-(1-{2-[4-(4-bromophenyl)-3-ethylthiazol-2(3H)-ylidene]hydrazono}ethyl)-3-phenyl-1,3,4-thiadiazol-2(3H)-imine showed a remarkable activity against three cancer cell lines, when compared to the reference drug cisplatin. The products were also tested for antibacterial activity against S. aureuss, P. aeruginosa, and E. coli bacteria and antifungal activity against A. Niger and C. albicans fungi. 5-(1-{2-[4-(4-Methoxyphenyl)thiazol-2-yl]hydrazono}ethyl)-3-phenyl-1,3,4-thiadiazol-2(3H)-imine was found to be much more potent antibacterial agent than the other synthesized compounds.

中文翻译：

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作为潜在抗癌药物的新型噻二唑掺入氨基噻唑衍生物的合成、表征和生物学评价

摘要

合成了一系列新型噻二唑掺入的氨基噻唑衍生物，并通过 IR、¹ H NMR 和¹³ C NMR 光谱、ESI 质谱和元素分析进行​​了表征。通过MTT法测试所有合成的化合物对MCF-7、A549和HeLa人类癌细胞系的体外抗癌活性。5-(1-{2-[4-(4-硝基苯基)噻唑-2-基]亚肼基}乙基)-3-苯基-1,3,4-噻二唑-2(3H)-亚胺和5- ( 1-{2-[4-(4-溴苯基)-3-乙基噻唑-2(3H ) -亚基]亚肼基}乙基)-3-苯基-1,3,4-噻二唑-2(3H ) -亚胺与参考药物顺铂相比，它对三种癌细胞系表现出显着的活性。还测试了产品对金黄色 葡萄球菌、铜绿假单胞菌和大肠杆菌的抗菌活性，以及​​对尼日尔和白色念珠菌的抗真菌活性。5-(1-{2-[4-(4-甲氧基苯基)噻唑-2-基]亚肼基}乙基)-3-苯基-1,3,4-噻二唑-2(3 H)-亚胺被发现是比其他合成化合物更有效的抗菌剂。