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

Yazala Jyothsna Pragathi; Reddymasu Sreenivasulu; Deekala Veronica; Rudraraju Ramesh Raju

doi:10.1007/s13369-020-04626-z

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

Arab J Sci Eng. 2021;46(1):225-232. doi: 10.1007/s13369-020-04626-z. Epub 2020 May 22.

Authors

Yazala Jyothsna Pragathi¹, Reddymasu Sreenivasulu², Deekala Veronica¹, Rudraraju Ramesh Raju¹

Affiliations

¹ Department of Chemistry, Acharya Nagarjuna University, Nagarjuna Nagar, Andhra Pradesh 522510 India.
² Department of Chemistry, University College of Engineering (Autonomous), Jawaharlal Nehru Technological University, Kakinada, Andhra Pradesh 533 003 India.

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.

Keywords: 1,2,4-Thiadiazole; 1,2,4-Triazole; 3,5-Bis(pyridin-3-yl)-1,2,4-thiadiazole; Anticancer activity; Letrozole.