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SAR studies of differently functionalized 4 '-phenylchalcone based compounds as inhibitors of cathepsins B, H and L

机译：基于不同官能化的4'-苯基醌基的SAR研究作为组织蛋白酶B，H和L的抑制剂

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摘要

Conditions related to the elevated levels of cathepsin B [3.4.22.1], cathepsin H [3.4.22.16] and cathepsin L [3.4.22.15] in various cancerous, rheumatoid arthritis and tissue degenerative disorders motivate the design, synthesis and evaluation of compounds as cathepsin B, H and L inhibitors. In the present work we report the synthesis and analysis of 36 different compounds belonging to 4 related series as cathepsin B, H and L inhibitors. After a preliminary screening of the synthesized compounds as inhibitors to the hydrolysis of endogenous protein substrates at pH 5.0, their inhibitory effects were evaluated on cathepsins B, H and L. Kinetic studies were carried out to determine the inhibition constants. It was found that the compounds belonging to different classes affected the enzyme activity significantly, and the activity was greatly affected by the presence of substituents. Maximum inhibition was caused by 2b and 2g in the cases of cathepsin B and cathepsin L, and 4d in the case of cathepsin H, where K-i values of the order of 10(-8) M, 10(-9) M and 10(-6) M, respectively, were obtained. The results are correlated with the docking results.
机译：与各种癌症中的组织蛋白酶B [3.4.22.1]和组织素L [3.4.22.15]和组织退行性疾病的组织蛋白酶H [3.4.22.16]和组织退行性障碍相关的病症促进了化合物的设计，合成和评价组织蛋白酶B，H和L抑制剂。在本工作中，我们报道了属于4种相关系列的36种不同化合物的合成和分析为组织蛋白B，H和L抑制剂。在PH 5.0下将合成化合物作为抑制剂的初步筛选作为抑制剂，在pH5.0下进行内源性蛋白质底物的水解，对组织蛋白酶B，H和L的抑制作用进行了评估。进行动力学研究以确定抑制常数。结果发现，属于不同类别的化合物显着影响酶活性，并且通过取代基的存在大大影响了活性。在组织蛋白酶B和组织蛋白酶L的情况下，在组织蛋白酶B和组织蛋白酶H的情况下引起最大抑制，并且在组织蛋白蛋白H的情况下，其中ki值为10（-8）m，10（-9）m和10（分别获得-6）m。结果与对接结果相关联。

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  • 来源
    《RSC Advances》 |2015年第62期|共14页
  • 作者

    Ravish Indu; Raghav Neera;

  • 作者单位

    Kurukshetra Univ Dept Chem Kurukshetra 136119 Haryana India;

    Kurukshetra Univ Dept Chem Kurukshetra 136119 Haryana India;

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  • 正文语种 eng
  • 中图分类 化学;
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