Design, synthesis, anticancer evaluation, and molecular docking studies of 1,3,4-thiadiazole bearing 1,3,5-triazine-thiazoles

Abstract

A new library of 1,3,4-thiadiazole bearing 1,3,5-triazine-thiazole (9a–j) compounds have been designed, synthesized, and assessed for their in vitro anticancer applications against a panel of human cancer cell lines, including prostate cancer (PC3&DU-145), lung cancer (A549), and breast cancer (MCF-7) by using the MTT method. The results were expressed as IC50 µM. Most of the tested compounds displayed good to moderate activity and were compared with the standard compound etoposide. The IC₅₀ values ranged for synthesized compounds from 0.11 ± 0.078 to 10.6 ± 5.47 µM and etoposide showed values ranging from 1.97 ± 0.45 to 3.08 ± 0.135 µM. Among the evaluated compounds, five (9a, 9b, 9c, 9d, and 9e) were found to show more potent activity. Specifically, compound 9a displayed good activity.

Graphical Abstract

Keywords:

• MBX-2982
• thiazole
• 1,3,4-thiadiazole and anticancer activity

Acknowledgments

The authors are thankful to Acharya Nagarjuna University, Guntur, Andhra Pradesh for constant encouragement during this research program for providing basic research facility.

Conflict of interest

The authors declare that they have no competing interests.

Additional information

Funding

The authors are also grateful to the Deanship of Scientific Research, King Khalid University for the financial support [Grant No. RGP. 2/21/44].