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    Some novel 5-benzylidenethiazolo[3,2-b]-1,2,4-triazole-6(5H)-one derivatives in the battle against cancer: Design, synthesis and their biological activities
    (Elsevier B.V., 2025) Avcı, Ahmet; Aztopal, Nazlıhan; Gökhan Kelekçi, Nesrin; Ulukaya, Engin; Tozkoparan, Birsen
    Considering the significant biological potential and the privileged status of the 1,2,4-triazole-5-thione scaffold as one of the essential building blocks in medicinal chemistry, a novel series of 30 new hybrid compounds of 1,2,4-triazole and 5-benzylidenethiazolidinone ring systems, named 5-benzilidene-thiazolo[3,2-b][1,2,4]triazole-6(5H)-one, were designed and synthesized in an attempt to obtain antiproliferative agents and EGFR inhibitors. Synthesized thiazolo[3,2-b][1,2,4]triazole-6(5H)-ones were investigated for their potential cytotoxic properties by cell viability, cell cycle, and cell death analyses. Compounds that exhibited more selective anti-growth activity in A549 cells were further scrutinized, revealing an accumulation in the G1 phase. Notably, compound 6e demonstrated outstanding results and was found to induce apoptosis. Molecular docking studies indicated that the designed compounds could act as EGFR inhibitors. Indeed, compounds 6i and 6j inhibited cell growth prevented EGFR-specific phosphorylation, and thus downregulated EGFR signaling, and inhibited EGFR enzyme activity with IC50 values of 2.46 μM and 4.72 μM, respectively. Additionally, druglikeness and some pharmaceutical properties of the synthesized compounds were predicted. This study underscores the promising therapeutic potential of the novel thiazolo[3,2-b]-1,2,4-triazole derivatives as EGFR inhibitors. © 2024 Elsevier B.V.