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Bioorg Med Chem Lett. 2016 Feb 15;26(4):1282-6. doi: 10.1016/j.bmcl.2016.01.016. Epub 2016 Jan 9.

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

Author information

1
College of Phamacy, Dongguk University-Seoul, Goyang 10326, Republic of Korea; College of Life Sciences and Biotechnology, Korea University, Seoul 02841, Republic of Korea.
2
College of Life Sciences and Biotechnology, Korea University, Seoul 02841, Republic of Korea.
3
College of Phamacy, The Gatholic University of Korea, Bucheon 420-743, Republic of Korea.
4
Natural Medicine Reasearch Center, Korea Research Institute of Bioscience and Biotechnology, Chungbuk 363-883, Republic of Korea.
5
College of Phamacy, Dongguk University-Seoul, Goyang 10326, Republic of Korea.
6
College of Life Sciences and Biotechnology, Korea University, Seoul 02841, Republic of Korea. Electronic address: ychoi@korea.ac.kr.

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.

KEYWORDS:

IL-6 antagonists; IL-6 signaling inhibitor; Oxazolidinone; Rheumatoid arthritis; STAT3; gp130

PMID:
26810262
DOI:
10.1016/j.bmcl.2016.01.016
[Indexed for MEDLINE]

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