ArticleAnti-cancer agents in medicinal chemistry2025
Urea and Thiourea Derivatives of Salinomycin as Agents Targeting Malignant Colon Cancer Cells.
Article in Anti-cancer agents in medicinal chemistry, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers.
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2 citing papers in PubMed.
- Mitochondrial-Targeted Triphenylphosphonium-Conjugated Ionophores with Enhanced Cytotoxicity in Cancer Cells.Molecules (Basel, Switzerland) · 2025Article
- Role of Natural Compounds as Anti-Cancer Agents.Anti-cancer agents in medicinal chemistry · 2025Article
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Authors and funding
4 authors.
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Abstract
backgroundSince it was discovered that a natural polyether ionophore called salinomycin (SAL) selectively inhibits human cancer cells, the scientific world has been paying special attention to this compound. It has been studied for nearly 15 years.
objectiveThus, a very interesting research direction is the chemical modification of SAL structure, which could give more biologically active agents.
methodsWe evaluated the anticancer activity of (thio)urea analogues class of C20-epi-aminosalinomycin (compound 3b). The studies covered the generation of reactive oxygen species (ROS), proapoptotic activity, cytotoxic activity, and lipid peroxidation
resultsThioureas 5a-5d showed antiproliferative activity against selected human colon cancer cell lines greater than that of chemically unmodified SAL, with a 2~10-fold higher potency towards a metastatic variant of colon cancer cells (SW620). Mechanistically, SAL derivatives showed proapoptotic activity in primary colon cancer cells and induced the production of reactive oxygen species (ROS) in these cells. In SW620 cells, SAL derivatives increased lipid peroxidation with a weak effect on apoptosis and low ROS formation with cytotoxic effects followed by cytostatic ones, suggesting different modes of action of the compounds against primary and metastatic colon cancer cells.
conclusionThe results of this study suggested that urea and thiourea derivatives of SAL provide promising leads for the rational development of new anticancer active agents.
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