Synthesis And Activity Of Curcumin Derivatives

The pharmacological activity and the metabolism in animal of the curcumin was described in this paper. The mechanisms of anti-tumor and the research development of curcumin were briefly reviewed.Based on the analysis of the structural characteristics, the compounds were designed in order to improve its anti-tumor activity and slow the metabolic rate.20 compounds were synthesied and 18 of them were new compounds. The 9 curcumin-derived pyrazoles and 2 curcumin-derived isoxazoles were synthesized from vanillin via alkylation of the hydroxyl group, condensation reaction and ring-closing reaction.The curcumin was taken as lead compound, and 8 curcumin mannich base derivatives were designed and synthesized from curcumin via protection of the hydroxyl group, methylation, deprotection, mannich reaction and alkylation of the hydroxyl group. The synthetic methods for the intermediates were investigated and reasonable synthetic route was studied. The structures of synthesized compounds were identified by 1H-NMR spectra and MS spectra.Now the new curcumin derivatives and 3 intermediates were screened for their antitumor activity in vitro against K562 cells from human beings chronic myel-oid leukemia. Preliminary pharmacological results showed that 4 of the compounds possessed more potent antitumor activities than curcumin in vitro and IC50S were lower than curcumin.