Citation: Tang Yuting, Ding Na, Wu Zhilin, Ye Jiao, Shen Kun, Hu Aixi. Synthesis and Antitumor Activity of N-[4-(t-Butyl)-5-benzylthiazol-2-yl]amininoacetamides[J]. Chinese Journal of Organic Chemistry, ;2017, 37(3): 675-682. doi: 10.6023/cjoc201610018 shu

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

College of Chemistry and Chemical Engineering, Hunan University, Changsha 410082

Corresponding author: Hu Aixi, axhu@hnu.edu.cn
Received Date: 12 October 2016
Revised Date: 16 November 2016

Fund Project: the National Natural Science Foundation of China 21442014

Figures(6)

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.
- thiazoleacetamide,
- morpholine,
- synthesis,
- antitumor activity
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