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Thiazole- and 1,3,4-Thiadiazole-Based Hybrids: Synthesis and In Vitro Cytotoxicity Against Human Cancer Cell Lines
Emine Terzi1,2, Tuba Ozdemir Sanci2,3, Beyza Ecem Oz Bedir1,2
1Department of Medical Biology, Faculty of Medicine, Ankara Yildirim Beyazit University, Ankara, Türkiye.
Chemical Biology & Drug Design
|January 28, 2026
Summary
New thiazole and 1,3,4-thiadiazole compounds were investigated for anticancer effects. Compound 6e demonstrated significant cytotoxic and pro-apoptotic activity in bladder and lung cancer cells, with low toxicity to healthy cells.
Area of Science:
- Medicinal Chemistry
- Molecular Biology
- Pharmacology
Background:
- Existing cancer treatments face challenges like toxicity, low selectivity, and drug resistance.
- There is a continuous need for novel, effective, and safer anticancer agents.
Purpose of the Study:
- To synthesize and evaluate novel thiazole and 1,3,4-thiadiazole derivatives as potential anticancer agents.
- To investigate the detailed anticancer mechanisms of the most potent compound, 6e, in human bladder (HTB-9) and lung (A549) cancer cells.
Main Methods:
- Cytotoxicity was assessed using the WST-1 assay to determine IC50 values.
- Apoptosis was analyzed via Annexin V-FITC/PI staining and flow cytometry.
- Caspase-3/7 activity, cell cycle progression (G2/M phase arrest), and cell migration were evaluated.
- Molecular docking was performed to predict binding interactions with caspase-3.
Main Results:
- Compound 6e exhibited potent cytotoxic effects against HTB-9 (IC50 = 38.9 μM) and A549 (IC50 = 82.86 μM) cells.
- Compound 6e significantly induced apoptosis (early in HTB-9, late in A549) and increased caspase-3/7 activity in both cell lines.
- Cell cycle analysis revealed G2/M phase arrest, and wound healing assays showed reduced cell migration.
- Molecular docking indicated strong binding of compound 6e to caspase-3, supporting its pro-apoptotic mechanism.
- Compound 6e displayed low cytotoxicity in healthy BEAS-2B cells, suggesting selective anticancer action.
Conclusions:
- Compound 6e, a novel thiazole derivative, possesses significant anticancer properties.
- Its mechanism involves the induction of apoptosis, cell cycle arrest, and inhibition of cell migration.
- The compound's selectivity towards cancer cells over healthy cells makes it a promising candidate for further anticancer drug development.
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