Rational design, synthesis, and pharmacological properties of pyranochalcone derivatives as potent anti-inflammatory agents

► Two natural pyranochalcones and their derivatives were synthesized and evaluated for anti-inflammatory activities. ► 5b showed remarkable in vitro and in vivo anti-inflammatory activity comparable to indomethacin. ► Molecular docking was employed to investigate the binding mode of the significant inhibitor 5b. ► Structure-activity relationship is discussed.