Citation: Yan Longjia, Li Yongliang, Deng Minggao, Chen Anchao, Du Zhiyun, Dong Changzhi, Chen Huixiong. Design, Synthesis and Biological Activities of Compounds Containing 1, 3, 4-Oxadiazole or 1, 3, 4-Thiadiazole[J]. Chinese Journal of Organic Chemistry, ;2020, 40(3): 731-739. doi: 10.6023/cjoc201907052 shu

Design, Synthesis and Biological Activities of Compounds Containing 1, 3, 4-Oxadiazole or 1, 3, 4-Thiadiazole

a.
Faculty of Light Industry and Chemical Engineering, Guangdong University of Technology, Guangzhou, 510006, China
b.
Biomédicale, Université Paris Descartes, 75006 Paris, France
c.
Université Paris Diderot, 75013 Paris, France

Corresponding author: Chen Huixiong, huixiong.chen@parisdescartes.fr
Received Date: 30 July 2019
Revised Date: 21 September 2019
Available Online: 21 November 2019
Fund Project: the National Natural Science Foundation of China 21672043Project supported by the National Natural Science Foundation of China (No. 21672043)

Figures(4)

In order to find new anti-tumor drugs, a series of novel 1, 3, 4-oxadiazole and 1, 3, 4-thiadiazole derivatives were designed and synthesized. The target compounds were evaluated for antitumor activity in vitro on four human cancer cell lines including B-16 (skin melanoma cells), PC-3 (human prostate cancer cells), U87 (human primary glioblastoma cells) and A549 (human non-small cell lung cancer cells). The results displayed that some of the compounds had good activities, especially, 5-((6-(4-(2-hydroxyethyl)piperazin-1-yl)-2-methylpyrimidin-4-yl)amino)-N-(2-methoxyphenyl)-1, 3, 4-thiadiazole-2-carboxamide (8b) and 5-((6-(4-(2-hydroxyethyl)piperazin-1-yl)-2-methylpyrimidin-4-yl)amino)-N-(4-methoxyphenyl)-1, 3, 4-thiadiazole-2-carboxamide (8c) showed high antitumor activities against four cancer cell lines, which was better than dasatinib. These compounds were further studied for their possible target of tumor suppression.
- 1, 3, 4-oxadiazole,
- 1, 3, 4-thiadiazole,
- anti-cancer,
- Src inhibitor
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1.
沈阳化工大学材料科学与工程学院沈阳 110142