Chinese Journal of Applied Chemistry ›› 2017, Vol. 34 ›› Issue (8): 905-911.DOI: 10.11944/j.issn.1000-0518.2017.08.160420

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Synthesis and Antitumor Activity of Tetrahydroimidazo[2',1':2,3]thiazolo [5,4-c]piperdine Derivatives

KOU Lidong,WANG Wei()   

  1. School of Chemistry and Chemical Engineering,He'nan Engineering Laboratory of Chemical Pharmaceutical and Biomedical Materials,He'nan Normal University,Xinxiang,He'nan 453007,China
  • Received:2016-10-18 Accepted:2017-03-28 Published:2017-07-25 Online:2017-07-26
  • Contact: WANG Wei
  • Supported by:
    Supported by the Scientific and Technological Projects of Henan Province(No.122107000014)


A series of novel 5,6,7,8-tetrahydroimidazo[2',1':2,3]thiazolo [5,4-c]piperidines was synthesized through sequential amino protection, condensation, cyclization, and deprotection reactions using piperidone as the raw material. The structures of these compounds were confirmed by proton or carbon nuclear magnetic resonance(1H NMR, 13C NMR), mass spectrometry(MS) and elemental analysis. The antitumor activities of these compounds were evaluated in vitro, and the results indicated that these compounds had certain inhibitory activities against MCF-7 human breast cancer cells, and the inhibitory activity of compound 5a reached the level of strong potency with the half maximal inhibitory concentration(IC50) value of 8.6 μmol/L. It provides a reference for the antitumor activity of such compounds.

Key words: tetrahydroimidazo[2',1':2,3]thiazolo [5,4-c]piperidine, derivatives, antitumor