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Chinese Journal of Organic Chemistry >

2012 , Vol. 32 >Issue 11: 2108 - 2114

DOI: https://doi.org/10.6023/cjoc201206018

Articles

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

  • Sun Liangpeng ,
  • Jiang Zhe ,
  • Gao Lixin ,
  • Li Yingzhe ,
  • Sun Liyun ,
  • Li Jia ,
  • Piao Huri
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  • 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 date: 2012-06-18

  Revised date: 2012-07-16

  Online published: 2012-07-19

Supported by

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

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Abstract

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 (4a～4n) 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

Cite this article

Sun Liangpeng , Jiang Zhe , Gao Lixin , Li Yingzhe , Sun Liyun , Li Jia , Piao Huri . Synthesis and Protein Tyrosine Phosphatase 1B Inhibitory Activity of Novel Chalcone Derivatives Containing 3,4-Dihydroquinolin-2(1H)-one Moiety[J]. Chinese Journal of Organic Chemistry, 2012 , 32(11) : 2108 -2114 . DOI: 10.6023/cjoc201206018

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