Concise Synthesis and Biological Evaluation of Chalcone Derivatives Bearing N-Heterocyclic Moieties

Abstract

In this study, we designed and synthesized a series of chalcone derivatives bearing N-heterocyclic moieties, and screened in vitro antiinflammatory in lipopolysaccharide (LPS)-stimulated RAW-264.7 macrophages and anticancer activity against a panel of human tumor cell lines. The results indicated that compound 9 not only had inhibitory effect on the generation of NO (IC50=8.11 μM) and significantly inhibited the production of TNF-α, but also showed better anticancer activity against Hela and SGC7901 (IC50=1.05 μM and 6.47 μM, respectively), which was identified as the most potent anti-inflammatory and anticancer agent.