Citation: Yan-Chun Guo, Jing Li, Jiao-Li Ma, Zhi-Ran Yu, Hai-Wei Wang, Wen-Juan Zhu, Xin-Cheng Liao, Yu-Fen Zhao. Synthesis and antitumor activity of α-aminophosphonate derivatives containing thieno[2,3-d]pyrimidines[J]. Chinese Chemical Letters, ;2015, 26(6): 755-758. doi: 10.1016/j.cclet.2015.03.026 shu

Synthesis and antitumor activity of α-aminophosphonate derivatives containing thieno[2,3-d]pyrimidines

1.
a The College of Chemistry and Molecular Engineering, The Key Laboratory of Chemical Biology and Organic Chemistry of Henan Province, Zhengzhou;
2.
University, Zhengzhou 450052, China;
3.
b Department of Chemistry, College of Chemistry and Chemical Engineering, The Key Laboratory for Chemical Biology of Fujian Province, Xiamen University, Xiamen 361005, China

Corresponding author: Xin-Cheng Liao,
Received Date: 13 November 2014
Available Online: 6 March 2015
Fund Project: This work was supported by the National Natural Sciences Foundations of China (Nos. 21171149, 21105091). (Nos. 21171149, 21105091)

Two series of thieno[2,3-d]pyrimidine derivatives were designed and synthesized, in which bioactive α-aminophosphonate subunits were introduced at the N3 position through an N-N bond connection. The in vitro cytotoxic activity of the novel compounds was tested against human esophageal carcinoma cells (EC109), human hepatocarcinoma cells (HepG2), human gastric carcinoma cells (MGC-803), respectively, by the MTT method. The evaluation results revealed that compounds 6mb, 6mf, 6mg, 6nd and 6nh exerted the most potent inhibition against HepG2, MGC-803 and EC109 cells, respectively. In particular, compound 6mg presented excellent inhibitory effect against HepG2 (91.2%) and MGC-803 (94.4%) cells.
- α-Aminophosphonate derivatives,
- Thieno[2,3-d]pyrimidine,
- Synthesis,
- Antitumor
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