Synthesis of Novel Thiazole Based 1,2,3-Triazole Derivatives as Inhibitors of Glioblastoma Cancer Cells

A library of thiazole – 1,2,3-triazole hybrids through the conventional 1,3-dipolar cycloaddition reaction of ethyl 2-(3-formyl-4-(prop-2-yn-1-yloxy) phenyl)-4-methylthiazole-5-carboxylate based alkyne via click reaction. Spectral data, such as IR, 1H-NMR, 13C-NMR, and Mass, were used to characterize the molecules structures. Synthesized compounds were screened for in vitro anticancer effects on human glioblastoma cell lines. Some compounds displayed potent activity with IC50 values of 10.67±0.94 µM, 4.72±3.92 µM, and 3.20±0.32 µM, in contrast to reference drug Temozolomide. Computational study against thymidylate synthase demonstrated favourable docking scores and binding interactions like H-bond, π-π stacked, and π-sulfur.

Synthesis of Novel Thiazole Based 1,2,3-Triazole Derivatives as Inhibitors of Glioblastoma Cancer Cells Keywords:

Cytotoxicity , Glioblastoma , Molecular docking , Thiazole , Triazole