Synthesis and Biological Evaluation of Novel Substituted Chalcone-piperazine Derivatives

A series of novel substituted chalcone-piperazine derivatives have been synthesized, and screened in vitro anti-inflammatory in lipopolysaccharide (LPS)-stimulated RAW-264.7 macrophages and cytotoxic activity against 3 strains human tumor cell lines. The results demonstrated that the substituents of the core ring and the NH group of piperazine ring had obvious influences on biological activities. Especially, 3,4,5-trimethoxy-4'-[N-(2-oxopropyl)-1-piperazinyl] chalcone (11) showed better inhibitory effect on the generation of NO (IC50 = 3.81 tmol/L), and 4-bromo-4'-[N-(4'-methyl-2-oxophenylethyl)-l-piperazinyl] chalcone (25) displayed good cytotoxic activity against A549, Hela and sk-ov-3 (IC50 = 0.54, 0.05 and 9.12 mu mol/L, respectively).