Citation: KOU Lidong, WANG Wei. Synthesis and Antitumor Activity of Tetrahydroimidazo[2', 1':2, 3]thiazolo[5, 4-c]piperdine Derivatives[J]. Chinese Journal of Applied Chemistry, ;2017, 34(8): 905-911. doi: 10.11944/j.issn.1000-0518.2017.08.160420 shu

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

KOU Lidong ,
WANG Wei ^,

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

Corresponding author: WANG Wei, weiwang161718@163.com
Received Date: 18 October 2016
Revised Date: 27 December 2017
Accepted Date: 28 March 2017

Fund Project: Supported by the Scientific and Technological Projects of Henan Province(No.122107000014)the Scientific and Technological Projects of Henan Province No.122107000014

Figures(1)

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