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高等学校化学研究 ›› 2009, Vol. 25 ›› Issue (4): 474-479.

• Articles • 上一篇    下一篇

Synthesis and Antiproliferative Activity of Novel [1,2,4]Triazolo[1,5-a]pyrimidine-7-amine Derivatives

ZHAI Xin, ZHANG Cun-long, HE Lei, LI Qi, WANG Jiu-liang, SHEN Xiao-li and GONG Ping*   

  1. Key Laboratory of New Drugs Design and Discovery of Liaoning Province, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, P. R. China
  • 收稿日期:2008-05-05 修回日期:2008-09-01 出版日期:2009-07-25 发布日期:2009-10-16
  • 通讯作者: GONG Ping. E-mail: gongpinggp@126.com

Synthesis and Antiproliferative Activity of Novel [1,2,4]Triazolo[1,5-a]pyrimidine-7-amine Derivatives

ZHAI Xin, ZHANG Cun-long, HE Lei, LI Qi, WANG Jiu-liang, SHEN Xiao-li and GONG Ping*   

  1. Key Laboratory of New Drugs Design and Discovery of Liaoning Province, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, P. R. China
  • Received:2008-05-05 Revised:2008-09-01 Online:2009-07-25 Published:2009-10-16
  • Contact: GONG Ping. E-mail: gongpinggp@126.com

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Abstract:

A series of novel N-anilino-2-substituted-5-methyl-[1,2,4]triazolo[1,5-a]pyrimidine-7-amine derivatives was prepared and evaluated for their in vitro antiproliferative activity against two cancer cell lines, Bel-7402 and HT-1080. Most of the compounds inhibited the cell proliferation at a low concentration. Seven compounds, VI5, VI7, VI10, and VI12―VI15, possessed marked antiproliferative activity superior to that of cisplatin. Of these seven initial hits, compound VI10 was the most active.

Key words: [1,2,4]Triazolo[1,5-a]pyrimidines; Antiproliferative activity; Anticancer