Sixteen novel hydroxytyrosol (HT) analogs with substitutions at the C-1 position of the HT aliphatic side chain were synthesized and evaluated for their cytostatic activity against MG-63 human osteoblast-like cells and for their antioxidant properties. The results revealed that these analogs exhibited significantly higher inhibitory activity compared with HT, which served as the positive control. Among these, the cyclo-substituted compounds stood out as particularly potent, demonstrating strong radical scavenging abilities and notable cytostatic effects against MG-63 cells. These findings suggest that the cyclo-substituted HT analogs hold considerable promise for the development of novel antioxidants with potential applications in bone physiology.

cite:Georgiou EA, Kalpaktsi I, Gioti K, Choleva M, Fragopoulou E, Skaltsounis AL, Tenta R, Kostakis IK. Synthesis of hydroxytyrosol analogs with enhanced antioxidant and cytostatic properties against MG-63 human osteoblast-like cells and their potential implications for bone health. Arch Pharm (Weinheim). 2024 Nov 16:e2400469. doi: 10.1002/ardp.202400469. Epub ahead of print. PMID: 39548899.