Department of Pharmaceutical Chemistry, Faculty of Pharmacy Anadolu University, 26470 EskişehirTurkey.
Doping and Narcotic Compounds Analysis Laboratory, Faculty of Pharmacy, Anadolu University 26470 Eskişehir, Turkey.
Acta Pharm. 2020 Dec 1;70(4):499-513. doi: 10.2478/acph-2020-0034.
The synthesis of new N-(5-substituted-1,3,4-thiadiazol-2-yl)-2-[(5-(substituted amino)-1,3,4-thiadiazol-2-yl)thio]acetamide derivatives and investigation of their anticancer activities were the aims of this work. All the new compounds' structures were elucidated by elemental analyses, IR, 1H NMR, 13C NMR and MS spectral data. Anticancer activity studies of the compounds were evaluated against MCF-7 and A549 tumor cell lines. In addition, with the purpose of determining the selectivity of cytotoxic activities, the most active compound was screened against a noncancer NIH3T3 cell line (mouse embryonic fibroblast cells). Among the tested compounds, compound 4y (N-(5-ethyl-1,3,4-thiadiazol-2-yl)-2-((5-(p-tolylamino)-1,3,4-thiadiazol-2-yl)thio)acetamide), showed promising cytotoxic activity against MCF7 cancer cell with an IC 50value of 0.084 ± 0.020 mmol L-1 and against A549 cancer cell with IC 50 value of 0.034 ± 0.008 mmol L-1, compared with cisplatin. The aromatase inhibitory activity was evaluated for compound 4y on MCF-7 cell line showing promising activity with IC50 of 0.062 ± 0.004 mmol L-1.
本工作旨在合成新型 N-(5-取代-1,3,4-噻二唑-2-基)-2-[(5-(取代氨基)-1,3,4-噻二唑-2-基)硫代]乙酰胺衍生物，并研究它们的抗癌活性。所有新化合物的结构均通过元素分析、IR、1H NMR、13C NMR 和 MS 谱数据进行了阐明。通过 MCF-7 和 A549 肿瘤细胞系评估了化合物的抗癌活性。此外，为了确定细胞毒性活性的选择性，对最活性化合物进行了筛选，以检测其对非癌细胞 NIH3T3 细胞系（小鼠胚胎成纤维细胞）的活性。在所测试的化合物中，化合物 4y（N-(5-乙基-1,3,4-噻二唑-2-基)-2-((5-(对甲苯胺基)-1,3,4-噻二唑-2-基)硫代)乙酰胺）对 MCF7 癌细胞具有有希望的细胞毒性活性，IC50 值为 0.084 ± 0.020 mmol L-1，对 A549 癌细胞的 IC50 值为 0.034 ± 0.008 mmol L-1，与顺铂相比。还评估了化合物 4y 对 MCF-7 细胞系的芳香酶抑制活性，表现出有希望的活性，IC50 为 0.062 ± 0.004 mmol L-1。
