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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

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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

    • 通讯作者: Xin-Cheng Liao,
  • 基金项目:

    This work was supported by the National Natural Sciences Foundations of China (Nos. 21171149, 21105091). (Nos. 21171149, 21105091)

摘要: 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.

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  • 发布日期:  2015-03-28
  • 收稿日期:  2014-11-13
  • 网络出版日期:  2015-03-06
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