期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 108, 期 -, 页码 586-593出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2015.12.020
关键词
Immunosuppressant; Molecular docking; Oxime ethers; PI3K gamma; Pyrazole
资金
- National Natural Science Foundation of China [21302002]
- Anhui Provincial Natural Science Foundation [1408085QB33, 1508085MB33]
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 mu M for lymph node cells and IC50 = 0.28 mu M for PI3K gamma), 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. (C) 2015 Elsevier Masson SAS. All rights reserved.
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