Design, Synthesis, and Evaluation of Bis-Chalcones and Bis-Flavones as Selective COX-2 Inhibitors.

ABSTRACT: Over the past two decades, the search for safe and effective COX-2 inhibitors has spurred extensive research on flavonoids. Within this context, synthetic flavonoid dimers have emerged as a promising subclass with potential anti-inflammatory activity. To investigate whether dimerization enhances their potency and selectivity, novel A-fused bis-chalcones and A-fused bis-flavones were synthesized and evaluated for their inhibitory activity against isolated human COX-1 and COX-2 enzymes, as well as their effects on prostaglandin E₂ production in whole human blood. Interestingly, the most active compound identified was a monomeric chalcone sharing the same substitution pattern as the top-performing bis-chalcone, suggesting that key structural features drive activity regardless of di

SUBMITTER: Pereira R 

PROVIDER: S-EPMC12949472 | biostudies-literature | 2026 Mar

REPOSITORIES: biostudies-literature