HETEROCYCLES

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

Zewei Mao, Xi Zheng, Yuping Lin, Yan Qi, Chunyan Hu, Chunping Wan,* and Gaoxiong Rao*

*Central laboratory, The NO.1 Affiliated Hospital of Yunnan University of Traditional Chinese Medicine, Kunming, 650021, China

Abstract

In this study, we designed and synthesized a series of chalcone derivatives bearing N- heterocyclic moieties, and screened in vitro anti- inflammatory 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=8.11μM) and significantly inhibited the production of TNF-α, but also showed better anticancer activity against Hela and SGC7901 (IC50=1.05μM and 6.47μM, respectively), which was identified as the most potent anti-inflammatory and anticancer agent.