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Novel pyrazole fused heterocyclic ligands: Synthesis, characterization, DNA binding/cleavage activity and anti-BVDV activity

Chao Han ,  Yan-Chun Guo ,  Dan-Dan Wang ,  Xing-Jie Dai ,  Feng-Juan Wu ,  Huan-Fei Liu ,  Gui-Fu Dai ,  Jing-Chao Tao

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Citation:  Chao Han, Yan-Chun Guo, Dan-Dan Wang, Xing-Jie Dai, Feng-Juan Wu, Huan-Fei Liu, Gui-Fu Dai, Jing-Chao Tao. Novel pyrazole fused heterocyclic ligands: Synthesis, characterization, DNA binding/cleavage activity and anti-BVDV activity[J]. Chinese Chemical Letters, 2015, 26(5): 534-538. doi: 10.1016/j.cclet.2015.01.006 shu

Novel pyrazole fused heterocyclic ligands: Synthesis, characterization, DNA binding/cleavage activity and anti-BVDV activity

    • 通讯作者: Gui-Fu Dai,
    Jing-Chao Tao,
摘要: A series of novel pyrazole fused heterocyclic derivatives were synthesized via a two-step procedure or a one-pot two step method, and their catalytic DNA cleavage abilities and anti-BVDV activities were also evaluated. The results obtained indicated that compounds 3b-3c could catalyze the cleavage of supercoiled DNA (pUC 19 plasmid DNA) to nicked DNA under physiological conditions with high yields via a hydrolytic mechanism. The studies on anti-viral activities against bovine viral diarrhea virus (BVDV) demonstrated that some of the pyrazole derivatives showed pronounced anti-BVDV activity with interesting EC50 values and no significant cytotoxicity. Among them, compound 3l showed the highest antiviral activity (EC50 = 0.12 μmol/L) and was 10 fold more than that of the positive control ribavirin (EC50 = 1.3 μmol/L), which provided a potential candidate for the development of anti-BVDV agents.

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  • 发布日期:  2015-01-10
  • 收稿日期:  2014-11-06
  • 网络出版日期:  2014-12-12
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