<abstract xmlns="http://www.w3.org/1999/xhtml">The synthesis of new <italic>N</italic>-(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 <bold>4y</bold> (<italic>N</italic>-(5-ethyl-1,3,4-thiadiazol-2-yl)-2-((5-(<italic>p</italic>-tolylamino)-1,3,4-thiadiazol-2-yl)thio)acetamide), showed promising cytotoxic activity against MCF7 cancer cell with an <italic>IC</italic>50value of 0.084 ± 0.020 mmol L−1 and against A549 cancer cell with <italic>IC</italic>50 value of 0.034 ± 0.008 mmol L−1, compared with cisplatin. The aromatase inhibitory activity was evaluated for compound <bold>4y</bold> on MCF-7 cell line showing promising activity with <italic>IC</italic>50 of 0.062 ± 0.004 mmol L−1.</abstract>

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 IC50value of 0.084 ± 0.020 mmol L−1 and against A549 cancer cell with IC50 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.

Synthesis and biological evaluation of novel 1,3,4-thiadiazole derivatives as possible anticancer agents

Doping and Narcotic Compounds Analysis Laboratory

Department of Pharmaceutical Toxicology, Faculty of Pharmacy

Acta Pharmaceutica

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 3.0 License.

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...

Synthesis and biological evaluation of novel 1,3,4-thiadiazole derivatives as possible anticancer agents

Publié en ligne: 13 mai 2020

Pages: 499 - 513

Accepté: 19 nov. 2019

DOI: https://doi.org/10.2478/acph-2020-0034

Mots clés
1, 3, 4-thiadiazole, anticancer activity, aromatase inhibitory activity, MTT assay

© 2020 Ulviye Acar Çevik et al., published by Sciendo

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 3.0 License.

Synthesis and biological evaluation of novel 1,3,4-thiadiazole derivatives as possible anticancer agents

Publié en ligne: 13 mai 2020

Pages: 499 - 513

Accepté: 19 nov. 2019

DOI: https://doi.org/10.2478/acph-2020-0034

Mots clés1, 3, 4-thiadiazole, anticancer activity, aromatase inhibitory activity, MTT assay

© 2020 Ulviye Acar Çevik et al., published by Sciendo

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 3.0 License.

Mots clés
1, 3, 4-thiadiazole, anticancer activity, aromatase inhibitory activity, MTT assay