摘要
以4-哌啶酮为原料,经过胺基保护、缩合、环合、脱保护等步骤,设计合成了一系列新型的5,6,7,8-四氢咪唑并[2',1':2-3]噻吩并[5,4-c]哌啶类化合物。通过核磁共振波谱仪(~1H NMR、^(13)C NMR)、质谱(MS)和元素分析确证了其结构。对其体外活性研究发现,该类化合物对乳腺癌细胞MCF-7具有一定的抑制活性,其中化合物5a的抑制活性最为显著,半数抑制浓度(IC_(50))值达到了8.6μmol/L。为此类化合物的抗肿瘤活性研究提供了参考。
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, 13 C NMR）, mass spectrometry （MS） and elemental analysis. The antitumor activities of these compounds were evaluated in vitro, and the resuhs indicated that these compounds had certain inhibitory activities against MCF-7 human breast cancer cells, and the inhibitory activity of 5a reached the level of strong potency with the half maximal inhibitory concentration （ICs0） 8.6 μmol/L. It provides a reference for the antitumor activitv of such comnounds. compound value of
作者
寇丽栋
王伟
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, Chin)
出处
《应用化学》
CSCD
北大核心
2017年第8期905-911,共7页
Chinese Journal of Applied Chemistry
基金
河南省科技攻关项目(122107000014)资助~~
