ELABORATION OF CURCUMIN INTO DIKETONE MODIFIED ANALOGUES DEVOID OF NUCLEOPHILIC ADDITION CAPABILITY; IMPLICATIONS FOR THEIR ANTITUMOR AND CHEMOSENSITIZING ACTIVITIES

Curcumin (CUR), a polyphenolic compound extracted from Curcuma longa L.,can beconsidered as a good lead compound for the design of new drugs for the treatment of cancer and other therapeutic purposes. CUR is endowed with a diketone function, which appears to be important for its antitumor activity: also depending on the dose, the compound may show complex either pro-oxidant or anti-oxidant effects, which both may, at least in part, be linked to this structural moiety. In the lower concentration, "chemopreventive", range, CUR behaves mainly as an antioxidant; at higher concentrations, the a, b-unsaturated 1,3-diketone, as a Michael acceptor, can form adducts with the –SH groups and generate …

Design and synthesis of hybrid drugs based on curcumin scaffold