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Title | Structure-activity relationship study of a series of novel oxazolidinone derivatives as IL-6 signaling blockers |
Authors | 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 |
Publisher | Elsevier |
Issue Date | 2016 |
Citation | Bioorganic & Medicinal Chemistry Letters, vol. 26, no. 4, pp. 1282-1286 |
Keywords | gp130; IL-6 antagonists; IL-6 signaling inhibitor; Oxazolidinone; Rheumatoid arthritis; STAT3 |
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 | |
Appears in Collections | |
Registered Date |
2019-05-02 |
