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Dimerization enhances cytotoxicity and tumor/non-tumor cell selectivity of juglone

Gregor C. Mittag, Isabell Wiengarn, Niels V. Heise, Sophie Hoenke, Hans-Peter Deigner, René Csuk


The study investigates the biological activity of spaced juglone dimers derived from the reaction of juglone with dicarboxylic acid dichlorides of varying chain lengths. It builds upon the observation that dimeric structures can exhibit enhanced biological activity compared to their monomeric counterparts. The cytotoxic effects of the synthesized compounds were assessed against a range of human cancer cell lines and non-malignant fibroblasts. Results indicate that the cytotoxicity varied depending on the length of the spacer, with specific dimers showing significantly improved activity. Furthermore, these compounds demonstrated a higher selectivity towards cancer cell lines than non-malignant fibroblasts, suggesting potential for targeted anticancer therapy. 

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