چهارشنبه 20 خرداد 1405
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Background and Objective: Pancreatic cancer is one of the most aggressive cancers, requiring innovative chemotherapeutic treatments with increased selectivity and effectiveness.
Methods: A new heterocyclic derivatives of dihydroquinazolin, oxazepine, tetrazole, and thiazine through the Schiff base derivative D were synthesized. This research used FTIR and ^1H-NMR spectroscopy to study Schiff base-derived heterocyclic compounds having dihydroquinazolin, oxazepine, tetrazole, and thiazine moieties. To evaluate selectivity, the synthesised compounds were tested in vitro against PANC-1 and HDFn cells.
Results: The compounds inhibited proliferation dose-dependently in MTT assays. Derivative D4 exhibited greater selectivity for cancer cells, (IC₅₀ = 129.5 µg/mL for PANC-1 and 237.4 µg/mL for HDFn cells), whereas derivative D5 exhibited stronger but less selective cytotoxicity (IC₅₀ = 68.9 and 61.01 µg/mL for PANC-1 and HDFn cells Due to increased nuclear intensity and membrane permeability, high-content screening of D4 decreased viable cell count and mitochondrial membrane potential. Caspase-8 and 9 activity significantly enhanced at 100 and 200 µg/mL (P = 0.0019 and P < 0.0001), indicating intrinsic and extrinsic apoptosis induction.
Conclusion: These findings suggest that Schiff base–derived heterocycle structural alteration optimization for tumor selectivity and biological safety may provide anticancer benefits.
Methods: A new heterocyclic derivatives of dihydroquinazolin, oxazepine, tetrazole, and thiazine through the Schiff base derivative D were synthesized. This research used FTIR and ^1H-NMR spectroscopy to study Schiff base-derived heterocyclic compounds having dihydroquinazolin, oxazepine, tetrazole, and thiazine moieties. To evaluate selectivity, the synthesised compounds were tested in vitro against PANC-1 and HDFn cells.
Results: The compounds inhibited proliferation dose-dependently in MTT assays. Derivative D4 exhibited greater selectivity for cancer cells, (IC₅₀ = 129.5 µg/mL for PANC-1 and 237.4 µg/mL for HDFn cells), whereas derivative D5 exhibited stronger but less selective cytotoxicity (IC₅₀ = 68.9 and 61.01 µg/mL for PANC-1 and HDFn cells Due to increased nuclear intensity and membrane permeability, high-content screening of D4 decreased viable cell count and mitochondrial membrane potential. Caspase-8 and 9 activity significantly enhanced at 100 and 200 µg/mL (P = 0.0019 and P < 0.0001), indicating intrinsic and extrinsic apoptosis induction.
Conclusion: These findings suggest that Schiff base–derived heterocycle structural alteration optimization for tumor selectivity and biological safety may provide anticancer benefits.
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