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

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• 作者：Sarbjit Singh^a ; ^b ; ^&dagger ; ; Veeraswamy Gajulapati^b ; ^&dagger ; ; Kondaji Gajulapati^b ; Ja-Il Goo^b ; Yeon-Hwa Park^c ; Hwa Young Jung^b ; Sung Yoon Lee^b ; Jung Ho Choi^d ; Young Kook Kim^d ; Kyeong Lee^a ; Tae-Hwe Heo^c ; Yongseok Choi^b ; ^{ychoi@korea.ac.kr" class="auth_mail" title="E-mail the corresponding author}
• 关键词：Rheumatoid arthritis ; IL-6 antagonists ; IL-6 signaling inhibitor ; STAT3 ; gp130 ; Oxazolidinone
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2016
• 出版时间：15 February 2016
• 年：2016
• 卷：26
• 期：4
• 页码：1282-1286
• 全文大小：1212 K

文摘

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.