Chin. J. Org. Chem. ›› 2017, Vol. 37 ›› Issue (3): 675-682.DOI: 10.6023/cjoc201610018 Previous Articles     Next Articles



唐玉婷, 丁娜, 伍智林, 叶姣, 申坤, 胡艾希   

  1. 湖南大学化学化工学院 长沙 410082
  • 收稿日期:2016-10-12 修回日期:2016-11-16 发布日期:2016-11-29
  • 通讯作者: 胡艾希,
  • 基金资助:


Synthesis and Antitumor Activity of N-[4-(t-Butyl)-5-benzylthiazol-2-yl]amininoacetamides

Tang Yuting, Ding Na, Wu Zhilin, Ye Jiao, Shen Kun, Hu Aixi   

  1. College of Chemistry and Chemical Engineering, Hunan University, Changsha 410082
  • Received:2016-10-12 Revised:2016-11-16 Published:2016-11-29
  • Contact: 10.6023/cjoc201610018
  • Supported by:

    Project supported by the National Natural Science Foundation of China (No. 21442014).

The antitumor activity research of N-(thiazol-2-yl) amide derivatives has been the focus of scholars. Physiologi-cally active substances containing amines widely exist in nature. A series of novel N-(4-(t-butyl)-5-benzylthiazol-2-yl) aminoacetamides were synthesized, and their structures were confirmed by 1H NMR, 13C NMR and elemental analysis. These compounds were evaluated for their in vitro anticancer activity on A549, Hela and MCF-7 cells. Most of the investigated compounds exhibited broad-spectrum antitumor activity. Compound 1t displayed significant activity against Hela cancer cells with IC50 value of (6.4±2.2) μmol/L. The AO/EB staining and cell cycle experiments were carried out on the preferred com-pound 1t. The result showed that compound 1t could significantly induce apoptosis of tumor cells and arrest the Hela cells in the S phase.

Key words: thiazoleacetamide, morpholine, synthesis, antitumor activity