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Design, Synthesis, and Biological Evaluation of 1,2,4-Thiadiazole-1,2,4-Triazole Derivatives Bearing Amide Functionality as Anticancer Agents.

ABSTRACT: A novel library of amide functionality having 1,2,4-thiadiazole-1,2,4-triazole (8a-j) analogs was designed, synthesized, and structures were characterized by 1H NMR, 13C NMR, and mass (ESI-MS) spectral data. Further, all compounds were evaluated for their anticancer activities against four different cancer cell lines including breast cancer (MCF-7, MDA MB-231), lung cancer (A549), and prostate cancer (DU-145) by MTT reduction assay method, and etoposide acts as a standard drug. The results confirmed that majority of the synthesized compounds showed moderate to potent anticancer activities aligned with four cell lines. Among the synthesized compounds, 8b, 8c, 8d, 8e, 8g and 8i displayed more potent activity along with inhibitory concentration values ranging from 0.10?±?0.084 to 11.5?±?6.49 µM than the standard IC50 values, which ranges from 1.91?±?0.84 to 3.08?±?0.135 µM, respectively.

SUBMITTER: Pragathi YJ 

PROVIDER: S-EPMC7243954 | biostudies-literature | 2020 May

REPOSITORIES: biostudies-literature

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Design, Synthesis, and Biological Evaluation of 1,2,4-Thiadiazole-1,2,4-Triazole Derivatives Bearing Amide Functionality as Anticancer Agents.

Pragathi Yazala Jyothsna YJ   Sreenivasulu Reddymasu R   Veronica Deekala D   Raju Rudraraju Ramesh RR  

Arabian journal for science and engineering 20200522 1

A novel library of amide functionality having 1,2,4-thiadiazole-1,2,4-triazole (<b>8a-j</b>) analogs was designed, synthesized, and structures were characterized by <sup>1</sup>H NMR, <sup>13</sup>C NMR, and mass (ESI-MS) spectral data. Further, all compounds were evaluated for their anticancer activities against four different cancer cell lines including breast cancer (MCF-7, MDA MB-231), lung cancer (A549), and prostate cancer (DU-145) by MTT reduction assay method, and etoposide acts as a sta  ...[more]

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