|
1,4 - pentadiene -3 - ketone analogues with curcumin structure similar to a variety of biological activity , mainly as antibacterial , anti-cancer , anti-inflammatory , antioxidant . Curcumin as a lead compound for about material development , has become a hot research field of drug . In addition, the structure of the compounds containing phenol ether and carbonate has high efficiency , low toxicity characteristics , has been widespread concern . To looking into the higher activity of curcumin derivatives according to the sub-structure connection method and biological isostere principle , the introduction of ether and carbonate structure in the 1,4 - pentadiene-3 - ketone structure , design , synthesis three categories new compounds , they are 14 asymmetric 1,5 - substituted aryl - 1 ,4 - pentadiene-3 - ketone compound ( IA ) , the structural change in three of the hydroxyl groups on the benzene ring asymmetric 1,5 - di - substituted aryl - 1 ,4 - pent- diene-3 - ketone compound ( IB ) , 3 - ethyl phenyl carbonate esters of compound ( II ) . All structures were the 1 H NMR 13 C NMR , IR and elemental analysis of conclusive evidence . The growth rate target compounds antibacterial activity test , most of the compounds have antibacterial activity . 50μg/mL concentration , compound IA 3 the IA 9 < / sub > the IA 11 and IA , 14 wheat red the mildew pathogen inhibition rates were 40.8% , 41.8% , 43.6 % and 51.6% , respectively , the control the pharmaceutical hymexazol ( 61.2% ) inhibitory effect : the compound IA 3 < / sub > , IA < / sub> IA 12 the Fusarium oxysporum inhibition rate were 32.5% , 50.3% and 32.9% , considerable control the pharmaceutical hymexazol ( 60.2% ) inhibitory effect of apples rot bacteria inhibition rates were 33.2% , 40.0% and 34.2% , respectively , with the control the pharmaceutical hymexazol ( 57.3% ) inhibitory effect quite . The PC3 cell models using the MTT assay anti-tumor activity in vitro testing of the target compounds , including compounds IA 3 < / sub> IA 4 < / sub> IA < / sub>, IA 7 , IA 10 and IA of 14 < / sub > has a certain anti - PC3 cell activity in vitro , 10μmol / L concentration of PC3 cells the role of 72 h, in vitro inhibitory activity were 83.7% , 87.2% , 87.8% , 83.9% , 88.5% and 82.2% , with the inhibitory effect of the positive control agent doxorubicin ( 97.7% ) quite .
|