Chin. J. Org. Chem. ›› 2018, Vol. 38 ›› Issue (3): 684-691.DOI: 10.6023/cjoc201707034 Previous Articles     Next Articles



高慧a, 郑喜b, 朱萍a, 王斯a, 万春平b, 饶高雄a, 毛泽伟a   

  1. a 云南中医学院中药学院 昆明 650500;
    b 云南中医学院第一附属医院中心实验室 昆明 650021
  • 收稿日期:2017-07-30 修回日期:2017-10-24 发布日期:2017-11-15
  • 通讯作者: 万春平,;毛泽伟,;
  • 基金资助:


Synthesis and Biological Evaluation of Novel Substituted Chalcone-piperazine Derivatives

Gao Huia, Zheng Xib, Zhu Pinga, Wang Sia, Wan Chunpingb, Rao Gaoxionga, Mao Zeweia   

  1. a College of Pharmaceutical Science, Yunnan University of Traditional Chinese Medicine, Kunming 650500;
    b Central Laboratory, The NO.1 Affiliated Hospital of Yunnan University of Traditional Chinese Medicine, Kunming 650021
  • Received:2017-07-30 Revised:2017-10-24 Published:2017-11-15
  • Contact: 10.6023/cjoc201707034;
  • Supported by:

    Project supported by the National Natural Science Foundation of China (Nos. 81560620, 81460624), the Application Basic Research Program of Yunnan Province (No. 2014FZ078) and the Yunnan Provincial Science and Technology Department-Applied Basic Research Joint Special Funds of Yunnan University of Traditional Chinese Medicine[No. 2017FF117(-023)].

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 μmol/L), and 4-bromo-4'-[N-(4'-methyl-2-oxophenylethyl)-1-piperazinyl]chalcone (25) displayed good cytotoxic activity against A549, Hela and sk-ov-3 (IC50=0.54, 0.05 and 9.12 μmol/L, respectively).

Key words: chalcone-piperazine derivatives, anti-inflammatory activity, cytotoxic activity