Promising Anticancer Activity of Novel Hydroxyethyloxy and Bromo derivatives of Curcumin and Its Complexes with BF2.

Curcumin has long been used for health purposes and is currently attracting significant research interest. In this study, we present a series of curcumin derivatives featuring structural modifications, including methoxy groups, short alcohol chains, and bromine atoms. The cytotoxic activity of the compounds obtained was tested against BA/F3 wt, BA/F3 del52, BA/F3 ins5, K562, Jurkat, HCT-116, and MDA-MB-231 cell lines and non-cancerous Balb/3T3 fibroblast lines. The most promising compounds 2a, 6a, and 9a demonstrated anticancer activity comparable to that of doxorubicin, while exhibiting toxicity toward fibroblasts similar to natural curcumin. In addition, thanks to microscopic fluorescence analysis, a mechanism of action was proposed for the most active compounds against the HCT-116 cell line. Some compounds exhibit moderate or strong proapoptotic activity, while others are characterized by cytostatic activity. Studied compounds demonstrated the DNA-intercalation ability and increased the content of cellular ROS in treated HCT-116 cells.