Chemical Research in Chinese Universities ›› 2009, Vol. 25 ›› Issue (4): 474-479.

• Articles • Previous Articles     Next Articles

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

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