| Synthesis and antitumor activity of α-aminophosphonate derivatives containing thieno[2,3-d]pyrimidines |
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| 引用本文： | 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]. 中国化学快报, 2015, 26(6): 755-758. DOI: 10.1016/j.cclet.2015.03.026 |
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| 作者姓名： | 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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| 作者单位： | a The College of Chemistry and Molecular Engineering, The Key Laboratory of Chemical Biology and Organic Chemistry of Henan Province, Zhengzhou;University, Zhengzhou 450052, China;b Department of Chemistry, College of Chemistry and Chemical Engineering, The Key Laboratory for Chemical Biology of Fujian Province, Xiamen University, Xiamen 361005, China |
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| 基金项目： | This work was supported by the National Natural Sciences Foundations of China (Nos. 21171149, 21105091). |
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| 摘 要： | Two series of thieno[2,3-d]pyrimidine derivatives were designed and synthesized, in which bioactive a-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(Hep G2), 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 Hep G2, MGC-803 and EC109 cells, respectively. In particular, compound 6mg presented excellent inhibitory effect against Hep G2(91.2%) and MGC-803(94.4%) cells.
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| 收稿时间： | 2014-11-13 |
| 修稿时间： | 2015-03-06 |
Synthesis and antitumor activity of α-aminophosphonate derivatives containing thieno[2,3-d]pyrimidines |
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| 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 |
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| Authors: | 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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| Affiliation: | a The College of Chemistry and Molecular Engineering, The Key Laboratory of Chemical Biology and Organic Chemistry of Henan Province, Zhengzhou;University, Zhengzhou 450052, China;b Department of Chemistry, College of Chemistry and Chemical Engineering, The Key Laboratory for Chemical Biology of Fujian Province, Xiamen University, Xiamen 361005, China |
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| 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 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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| Keywords: | &alpha -Aminophosphonate derivatives Thieno[2,3-d]pyrimidine Synthesis Antitumor |
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