Structure–activity relationship study of a series of novel oxazolidinone derivatives as IL-6 signaling blockers. Issue 4 (15th February 2016)

• Record Type: Journal Article
• Authors: Singh, Sarbjit; Gajulapati, Veeraswamy; Gajulapati, Kondaji; Goo, Ja-Il; Park, Yeon-Hwa; Jung, Hwa Young; Lee, Sung Yoon; Choi, Jung Ho; Kim, Young Kook; Lee, Kyeong; Heo, Tae-Hwe; Choi, Yongseok
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 26:Issue 4(2016)
• Page Start: 1282
• Page End: 1286
• Publication Date: 2016-02-15
• Subjects: Rheumatoid arthritis -- IL-6 antagonists -- IL-6 signaling inhibitor -- STAT3 -- gp130 -- Oxazolidinone; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2016.01.016
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: 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, compound4d 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.