Synthesis of Dihydrothiophene Ureidoformamide Derivatives and Exploration of Their Potential Anticancer Activity.

Authors

Khawla Boudebbous, Arif Mermer, Tuğba Kul Köprülü, Dominique Harakat, Anthony Robert, Anthony Abou Dib, Houssem Boulebd

Published in

Journal of biochemical and molecular toxicology. Volume 40. Issue 7. Pages e70994.

Abstract

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.

PMID:
42371741
Bibliographic data and abstract were imported from PubMed on 30 Jun 2026.

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