Citation: Xin Zhai, Nan Jiang, Ke Liang Zhang, Feng Bao, Ping Gong. Design, synthesis and antiproliferative activity of novel 2,7-disubstituted triazolo[1,5-a]pyrimidines[J]. Chinese Chemical Letters, ;2009, 20(10): 1179-1182. doi: 10.1016/j.cclet.2009.04.027 shu

Design, synthesis and antiproliferative activity of novel 2,7-disubstituted triazolo[1,5-a]pyrimidines

Xin Zhai ^a, ,
Nan Jiang ^a ,
Ke Liang Zhang ^b ,
Feng Bao ^a ,
Ping Gong ^a

a Key Lab of New Drugs Design and Discovery of Liaoning Province, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, China;
b Liaoning Food and Drug Administration Technical Evaluation Center, Shenyang 110003, China

Received Date: 24 February 2009

In our efforts to identify novel potent anticancer agents, we synthesized a series of 2,7-disubstituted triazolo[1,5-a]pyrimidines (6-16).Their antiproliferative activity against Bel-7402, HT-1080 and WI-38 cell lines was tested by MTTassay in vitro.Four of the compounds (9-11 and 16) displayed promising antiproliferative activity superior to gefitinib, especially compound 9.A preliminary SAR study of these derivatives was performed.
- Triazolo[1,5-a]pyrimidines,
- Synthesis,
- Antiproliferative activity
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