Chin. J. Org. Chem. ›› 2012, Vol. 32 ›› Issue (11): 2108-2114.DOI: 10.6023/cjoc201206018 Previous Articles     Next Articles



孙良鹏a, 姜哲b, 高立信c, 李英哲a, 孙立云a, 李佳c, 朴虎日a   

  1. a 长白山生物资源与功能分子教育部重点实验室 延边大学药学院 延吉 133002;
    b 延边大学附属医院 延吉 133002;
    c 国家新药筛选中心 中国科学院上海药物研究所 上海 201203
  • 收稿日期:2012-06-18 修回日期:2012-07-16 发布日期:2012-07-19
  • 通讯作者: 李佳, 朴虎日;
  • 基金资助:

    国家自然科学基金(Nos. 20962021, 81125023)资助项目.

Synthesis and Protein Tyrosine Phosphatase 1B Inhibitory Activity of Novel Chalcone Derivatives Containing 3,4-Dihydroquinolin-2(1H)-one Moiety

Sun Liangpenga, Jiang Zheb, Gao Lixinc, Li Yingzhea, Sun Liyuna, Li Jiac, Piao Huria   

  1. a Key Laboratory of Natural Resources of Changbai Mountain & Functional Molecules, Ministry of Education, College of Pharmacy, Yanbian University, Yanji 133002;
    b Yanbian University Hospital, Yanji 133002;
    c National Center for Drug Screening, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203
  • Received:2012-06-18 Revised:2012-07-16 Published:2012-07-19
  • Supported by:

    Project supported by the National Natural Science Foundation of China (Nos. 20962021, 81125023).

Protein tyrosine phosphatase 1B (PTP1B) has recently been identified as new drug target for type II diabetes and obesity due to it is a negative regulator of the insulin and leptin-signaling pathway. In order to find new nonphosphonate-based pTyr mimetics, a series of novel chalcone derivatives bearing the 3,4-dihydroquinolin-2(1H)-one moieties (4a4n) were designed, synthesized, and evaluated for their PTP1B inhibitory activity. The results demonstrated that all compounds presented potent inhibitory activities against PTP1B, among which compounds 4e and 4i exhibited most potent with IC50 value of (4.64±0.38) and (4.36±0.41) μmol/L, respectively.

Key words: chalcone, 3,4-dihydroquinolin-2(1H)-one, PTP1B inhibitor