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

Authors
Singh, SarbjitGajulapati, VeeraswamyGajulapati, KondajiGoo, Ja-IlPark, Yeon-HwaJung, Hwa YoungLee, Sung YoonChoi, Jung HoKim, Young KookLee, KyeongHeo, Tae-HweChoi, Yongseok
Issue Date
15-Feb-2016
Publisher
PERGAMON-ELSEVIER SCIENCE LTD
Keywords
Rheumatoid arthritis; IL-6 antagonists; IL-6 signaling inhibitor; STAT3; gp130; Oxazolidinone
Citation
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.26, no.4, pp.1282 - 1286
Indexed
SCIE
SCOPUS
Journal Title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume
26
Number
4
Start Page
1282
End Page
1286
URI
https://scholar.korea.ac.kr/handle/2021.sw.korea/89517
DOI
10.1016/j.bmcl.2016.01.016
ISSN
0960-894X
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 mu M which was much better than (+)-Madindoline A (IC50 = 21 mu M), a known inhibitor of IL-6. (C) 2016 Elsevier Ltd. All rights reserved.
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