应用化学2017，Vol.34Issue(8)：905-911,7.DOI:10.11944/j.issn.1000-0518.2017.08.160420
四氢咪唑并[2′,1′:2,3]噻吩并[5,4-c]哌啶衍生物的合成及抗肿瘤活性
Synthesis and Antitumor Activity of Tetrahydroimidazo[2′,1′:2,3]thiazolo [5,4-c]piperdine Derivatives
摘要
Abstract
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.关键词
四氢咪唑并[2′,1′:2-3]噻吩并[5,4-c]哌啶/衍生物/抗肿瘤Key words
tetrahydroimidazo[2′/1′:2/3]thiazolo [5/4-c]piperidine/derivatives/antitumor分类
化学化工引用本文复制引用
寇丽栋,王伟..四氢咪唑并[2′,1′:2,3]噻吩并[5,4-c]哌啶衍生物的合成及抗肿瘤活性[J].应用化学,2017,34(8):905-911,7.基金项目
河南省科技攻关项目(122107000014)资助 （122107000014）
Supported by the Scientific and Technological Projects of Henan Province(No.122107000014) （No.122107000014）
