摘要：More than fifty chalcone derivatives were synthesized to examine structure-activity relationships against human aldose reductase. Certain 2', 4'-dihydroxychalcone derivatives inhibited human aldose reductase activities, and 2', 4', 2, 4-tetrahydroxychalcone and 2', 4', 2-trihydroxychalcone showed potent inhibitory activity with IC50 values of 7.4×10-9 M and 1.6×10-7 M, respectively. On the other hand, cis-form chalcones, which were isomerized from the original trans-forms by irradiation of daylight in methanol solution, promoted the activity of human aldose reductase.
