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

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

doi:10.1016/j.bmcl.2016.01.016

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

Singh, Sarbjit;
Gajulapati, Veeraswamy;
Gajulapati, Kondaji;
Goo, Ja-Il;
Park, Yeon-Hwa;
... Lee, Kyeong;
외 6명

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초록

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.

키워드

Rheumatoid arthritis; IL-6 antagonists; IL-6 signaling inhibitor; STAT3; gp130; Oxazolidinone; ACUTE-PANCREATITIS; GLYCOPROTEIN 130; MADINDOLINE-A; INTERLEUKIN-6; INHIBITION; ANTAGONIST; GP130

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

저자: 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

DOI: 10.1016/j.bmcl.2016.01.016

발행일: 2016-02-15

유형: Article

저널명: Bioorganic and Medicinal Chemistry Letters

권: 26

호: 4

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