Bis-chalcones: A review of synthetic methodologies and anti-inflammatory effects

• Published in: European journal of medicinal chemistry 2023-04, Vol.252, p.115280-115280, Article 115280
• Main Authors: Pereira, Rui, Silva, Artur M.S., Ribeiro, Daniela, Silva, Vera L.M., Fernandes, Eduarda
• Format: Article
• Language: English
• Subjects: Anti-Inflammatory Agents - pharmacology; Bis-chalcones; Chalcones - chemistry; Claisen–Schmidt condensation; Flavonoids; Green synthesis; Inflammation; Molecular Docking Simulation
• ISSN: 0223-5234; 1768-3254
• DOI: 10.1016/j.ejmech.2023.115280

Chalcones are bioactive molecules of natural and synthetic sources, whose physicochemical properties, reactivity, and biological activities are well-known among the scientific community. However, there are many molecules strictly related to chalcones with significantly less recognition like bis-chalcones. Several studies indicated that bis-chalcones have advantages over chalcones in specific bioactivities like anti-inflammatory activity. This review article describes the chemical structure and chemical properties of bis-chalcones, as well as the methods reported in the literature for the synthesis of these compounds highlighting the most recent developments. Finally, the anti-inflammatory activity of bis-chalcones is described, emphasizing the active structures found in literature and their mechanisms of action. [Display omitted] •Bis-chalcones are a subclass of chalcones that earned considerable interest.•Chemical synthesis of bis-chalcones based on established knowledge on chalcones.•Improvement of classic synthetic methodologies with new reaction conditions.•Very few bis-chalcones are associated with anti-inflammatory activity.•More studies on anti-inflammatory bis-chalcones are required to establish a SAR.