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Title 

Structure-activity relationship study of a series of novel oxazolidinone derivatives as IL-6 signaling blockers

Authors 

S SinghV GajulapatiK GajulapatiJ I GooY H ParkH Y JungS Y LeeJeong Ho ChoiYoung-Kook KimK LeeT H HeoY Choi

Publisher 

Elsevier

Issue Date 

2016

Citation 

Bioorganic & Medicinal Chemistry Letters, vol. 26, no. 4, pp. 1282-1286

Keywords 

gp130IL-6 antagonistsIL-6 signaling inhibitorOxazolidinoneRheumatoid arthritisSTAT3

Abstract 

A series of oxazolidinone and indole derivatives were synthesized and evaluated as IL-6 signaling blockers by measuring the effects of these compounds on IL-6-induced luciferase expression in human hepatocarcinoma HepG2 cells transfected with p-STAT3-Luc. Among different compounds screened, compound 4d was emerged as the most potent IL-6 signaling blockers with IC50 value of 5.9 μM which was much better than (+)-Madindoline A (IC50 = 21 μM), a known inhibitor of IL-6.

ISSN 

0960-894X

Link 

http://dx.doi.org/10.1016/j.bmcl.2016.01.016

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2019-05-02


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