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

Yan Chun Guo, Jing Li, Jiao Li Ma, Zhi Ran Yu, Hai Wei Wang, Wen Juan Zhu, Xin Cheng Liao, Yu Fen Zhao

Research output: Contribution to journalArticlepeer-review

38 Citations (Scopus)


Abstract 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 NN 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.

Original languageEnglish
Article number3255
Pages (from-to)755-758
Number of pages4
JournalChinese Chemical Letters
Issue number6
Publication statusPublished - 2015
Externally publishedYes


  • Antitumor
  • Synthesis
  • Thieno[2,3-d]pyrimidine
  • α-Aminophosphonate derivatives

ASJC Scopus subject areas

  • Chemistry(all)


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