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含O-苄基肟部分的(E)-1,3-二苯基-1H-吡唑衍生物作为潜在免疫抑制剂：设计、合成、分子对接及生物学评价

(E)-1,3-diphenyl-1H-pyrazole derivatives containing O-benzyl oxime moiety as potential immunosuppressive agents: Design, synthesis, molecular docking and biological evaluation.

作者信息

Lv Xian-Hai, Li Qing-Shan, Ren Zi-Li, Chu Ming-Jie, Sun Jian, Zhang Xin, Xing Man, Zhu Hai-Liang, Cao Hai-Qun

机构信息

College of Plant Protection, Anhui Agricultural University, Hefei 230036, PR China.

School of Medical Engineering, Hefei University of Technology, Hefei 230009, PR China.

出版信息

Eur J Med Chem. 2016 Jan 27;108:586-593. doi: 10.1016/j.ejmech.2015.12.020. Epub 2015 Dec 15.

DOI:10.1016/j.ejmech.2015.12.020
PMID:26720154
Abstract

A series of novel (E)-1,3-diphenyl-1H-pyrazole derivatives containing O-benzyl oxime moiety were firstly synthesized and their immunosuppressive activities were evaluated. Among all the compounds, 4n exhibited the most potent inhibitory activity (IC50 = 1.18 μM for lymph node cells and IC50 = 0.28 μM for PI3Kγ), which was comparable to that of positive control. Moreover, selected compounds were tested for their inhibitory activities against IL-6 released in ConA-simulated mouse lymph node cells, 4n exhibited the most potent inhibitory ability. Furthermore, in order to study the preliminary mechanism of the compounds with potent inhibitory activity, the RT-PCR experiment was performed to assay the effect of selected compounds on mRNA expression of IL-6. Among them, compound 4n strongly inhibited the expression of IL-6 mRNA.

摘要

首先合成了一系列含有O-苄基肟部分的新型（E）-1,3-二苯基-1H-吡唑衍生物，并评估了它们的免疫抑制活性。在所有化合物中，4n表现出最有效的抑制活性（淋巴结细胞的IC50 = 1.18 μM，PI3Kγ的IC50 = 0.28 μM），与阳性对照相当。此外，测试了所选化合物对ConA刺激的小鼠淋巴结细胞中释放的IL-6的抑制活性，4n表现出最有效的抑制能力。此外，为了研究具有强抑制活性的化合物的初步机制，进行了RT-PCR实验以测定所选化合物对IL-6 mRNA表达的影响。其中，化合物4n强烈抑制IL-6 mRNA的表达。

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