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Synthesis of Dihydrothiophene Ureidoformamide Derivatives and Exploration of Their Potential Anticancer Activity
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DOI：10.1002/jbt.70994.png)
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Abstract
En 中文
Dihydrothiophene ureidoformamide derivatives are sulfur-containing heterocyclic frameworks that remain relatively underexplored for their anticancer potential, despite possessing structural features that may enable interactions with biological targets involved in tumor progression. In the present study, a series of these derivatives was synthesized, structurally characterized, and evaluated for their anticancer activity against HCT116 human colorectal carcinoma cells. Among the tested compounds, compound 7 exhibited notable antiproliferative activity, showing a faster reduction in cell index compared to the reference drug paclitaxel during the initial 24 h of treatment, along with a dose-dependent decrease in cell index. Flow cytometric analysis using Annexin V-FITC/PI staining revealed that compound 7 induced significant apoptotic cell death, reaching 62.89% after 24 h of treatment. Molecular docking studies further indicated favorable binding interactions of compound 7 with several cancer-related targets, including EGFR, VEGFR-2, and AKT1. Overall, the obtained results suggest that this family of compounds, particularly compound 7, may represent an interesting scaffold for further investigation in the development of anticancer agents
Keywords:
anticancer activity
apoptosis
dihydrothiophene derivatives
HCT116 cells
molecular docking
ureidoformamide
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