关键词: 花旗松素衍生物, 查尔酮, 抗炎活性

Abstract: The 2'-hydroxyl chalcone derivatives 3a～3o were prepared by condensation of 2′-hydroxyhypnone derivatives and phenyl aldehyde derivatives under alkali.After oxidation and hydrolysis,A and /or B-ring substitut-ed taxifolins 4a-4o were obtained.Then C-ring varied taxifolins 4p～4r were synthesized by oxidative hy-drolysis of 2′-azyl chalcone derivatives 3p-3r,which were prepared by method above.19 compounds were synthesized and their structures were confirmed by 1H NMR and ¹³C NMR.To best of our knowledge,13 of them were unknown in the literature.The anti-inflammatory activity of synthesized compounds was evaluated against RAW264.7 cell in vitro.The preliminary results indicated that 4,4c,4i,4l and 4m showed good anti-inflammatory activity (P<0.001).Structure-activity relationship showed that the 5,7-dihydroxyl substitution located in the A-ring was critical for anti-inflammatory activity.The 4/-fluorine substitution located in the B-ring has excellent influence.The anti-inflammatory activity reduced or disappeared when C-ring was varied.

Key words: taxifolin derivatives, chalcone, anti-inflammatory activity