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

摘要

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