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

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Title
Structure-activity relationship study of a series of novel oxazolidinone derivatives as IL-6 signaling blockers
Author(s)
S Singh; V Gajulapati; K Gajulapati; J I Goo; Y H Park; H Y Jung; S Y Lee; Jeong Ho Choi; Young-Kook Kim; K Lee; T H Heo; Y Choi
Bibliographic Citation
Bioorganic & Medicinal Chemistry Letters, vol. 26, no. 4, pp. 1282-1286
Publication Year
2016
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.
Keyword
gp130IL-6 antagonistsIL-6 signaling inhibitorOxazolidinoneRheumatoid arthritisSTAT3
ISSN
0960-894X
Publisher
Elsevier
Full Text Link
http://dx.doi.org/10.1016/j.bmcl.2016.01.016
Type
Article
Appears in Collections:
1. Journal Articles > Journal Articles
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