Current medicinal chemistry · 2026
Synthesis, Characterization, Anti-Proliferative Activity, Cell Cycle Analysis, and Annexin V-FITC Apoptosis Study of New Thiazole Derivatives.
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Alshareef Hossa F
Аннотация
OBJECTIVE: We herein synthesized a new series of thiazole derivatives as anti- breast cancer agents.
METHODS: Different thiazole derivatives, 4 and 11, were synthesized and used to prepare new Schiff bases 5a-d and Mannich bases 9a-c. Their structures were confirmed based on their spectral data.
RESULTS: The biological activity results of the synthesized thiazole derivatives against breast cancer cells (MCF-7) revealed that three derivatives, 5a, 5b, and 11, exhibited superior activity, with IC50 values between 85.97 and 88.24 μM, compared to the reference drug cisplatin, which has an IC50 of 74.8 μM.The most active thiazole derivatives 5a, 5b, and 11 were subsequently assessed for cytotoxicity against noncancerous normal cells (WI-38 cells) to evaluate their safety. The results demonstrated that the MCF-7 cell line displayed heightened sensitivity to the three thiazoles, while none of the derivatives altered the morphology of normal WI-38 cells at any concentration, indicating their safety.
DISCUSSION: All three thiazole derivatives increased DNA content in the G2/M phase (33.12% for derivative 5a, 25.29% for derivative 5b, and 29.4% for derivative 11)-compared with control cells (7.54%) in cell cycle analysis. Furthermore, all three derivatives resulted in substantial elevations in the percentages of early, late, and total apoptotic cells, as well as an increase in the proportion of cells in the necrotic phase, rising from 2.14% in the control group to 4.34% in 5a and 3.73% in 5b.
CONCLUSION: The thiazole derivatives 5a, 5b, and 11 exhibited activities against CDK2, with IC50 values ranging from 1.05 μg/ml to 1.203 μg/ml. The pharmacokinetics and toxicity profiles of derivatives 5a, 5b, and 11 demonstrated that they possess low toxicity, are appropriate for oral bioavailability, and exhibit acceptable drug-like characteristics.
METHODS: Different thiazole derivatives, 4 and 11, were synthesized and used to prepare new Schiff bases 5a-d and Mannich bases 9a-c. Their structures were confirmed based on their spectral data.
RESULTS: The biological activity results of the synthesized thiazole derivatives against breast cancer cells (MCF-7) revealed that three derivatives, 5a, 5b, and 11, exhibited superior activity, with IC50 values between 85.97 and 88.24 μM, compared to the reference drug cisplatin, which has an IC50 of 74.8 μM.The most active thiazole derivatives 5a, 5b, and 11 were subsequently assessed for cytotoxicity against noncancerous normal cells (WI-38 cells) to evaluate their safety. The results demonstrated that the MCF-7 cell line displayed heightened sensitivity to the three thiazoles, while none of the derivatives altered the morphology of normal WI-38 cells at any concentration, indicating their safety.
DISCUSSION: All three thiazole derivatives increased DNA content in the G2/M phase (33.12% for derivative 5a, 25.29% for derivative 5b, and 29.4% for derivative 11)-compared with control cells (7.54%) in cell cycle analysis. Furthermore, all three derivatives resulted in substantial elevations in the percentages of early, late, and total apoptotic cells, as well as an increase in the proportion of cells in the necrotic phase, rising from 2.14% in the control group to 4.34% in 5a and 3.73% in 5b.
CONCLUSION: The thiazole derivatives 5a, 5b, and 11 exhibited activities against CDK2, with IC50 values ranging from 1.05 μg/ml to 1.203 μg/ml. The pharmacokinetics and toxicity profiles of derivatives 5a, 5b, and 11 demonstrated that they possess low toxicity, are appropriate for oral bioavailability, and exhibit acceptable drug-like characteristics.