Design,synthesis and antiproliferative activity of novel 2,7-disubstituted triazolo[1,5-a]pyrimidines |
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| Authors: | Xin Zhaia Nan Jianga Ke Liang Zhangb Feng Baoa Ping Gong a Key Lab of New Drugs Design Discovery of Liaoning Province School of Pharmaceutical Engineering Shenyang Pharmaceutical University Shenyang China b Liaoning Food Drug Administration Technical Evaluation Center Shenyang China |
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| Institution: | 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 |
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| Abstract: | In our efforts to identify novel potent anticancer agents, we synthesized a series of 2,7-disubstituted triazolo1,5-a]pyrimidines (6–16). Their antiproliferative activity against Bel-7402, HT-1080 and WI-38 cell lines was tested by MTT assay 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. |
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| Keywords: | Triazolo[1 5-a]pyrimidines Synthesis Antiproliferative activity |
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