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Design Synthesis and Biological Activities of Novel Pyrazole Oxime Compounds Containing a Substituted Pyridyl Moiety

机译:含取代的吡啶基部分的新型吡唑肟化合物的设计合成和生物活性

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摘要

In this paper, in order to find novel biologically active pyrazole oximes, a series of pyrazole oxime compounds bearing a substituted pyridyl unit were prepared. Bioassays showed that some target compounds were found to have good acaricidal activity against Tetranychus cinnabarinus at a concentration of 500 μg/mL, compound >9q especially displayed potent acaricidal activity against T. cinnabarinus when the concentration was reduced to 100 μg/mL. Interestingly, most target compounds possessed excellent insecticidal activities against Oriental armyworm at 500 μg/mL. Moreover, some compounds were active against Aphis medicaginis and Nilaparvata lugens at 500 μg/mL. Additionally, compounds >9b, >9g, >9l, >9p, >9q, >9r, >9s, >9t, >9u, and >9v displayed significant antiproliferative activities against HepG2 cells with IC50 values of 1.53–17.27 μM, better than that of the control 5-fluorouracil (IC50 = 35.67 μM).
机译:在本文中,为了找到新型的具有生物活性的吡唑肟,制备了一系列带有取代吡啶基单元的吡唑肟化合物。生物测定表明,在浓度为500μg/ mL时,发现一些目标化合物对朱砂叶螨有良好的杀螨活性,化合物> 9q 特别是当浓度降低至100时,对朱砂叶螨有较强的杀螨活性。微克/毫升有趣的是,大多数目标化合物以500μg/ mL的浓度具有出色的对东方粘虫的杀虫活性。此外,一些化合物对500 mg / mL的蚜虫和褐飞虱具有活性。此外,化合物> 9b ,> 9g ,> 9l ,> 9p ,> 9q , > 9r ,> 9s ,> 9t ,> 9u 和> 9v 对HepG2细胞显示出显着的抗增殖活性IC50值为1.53–17.27μM,优于对照5-氟尿嘧啶(IC50 = 35.67μM)。

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