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Structure-activity relationship study of a series of novel oxazolidinone derivatives as IL-6 signaling blockers
- 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
- Issue Date
- 15-Feb-2016
- Publisher
- PERGAMON-ELSEVIER SCIENCE LTD
- Keywords
- Rheumatoid arthritis; IL-6 antagonists; IL-6 signaling inhibitor; STAT3; gp130; Oxazolidinone
- Citation
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.26, no.4, pp 1282 - 1286
- Pages
- 5
- Indexed
- SCI
SCIE
SCOPUS
- Journal Title
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
- Volume
- 26
- Number
- 4
- Start Page
- 1282
- End Page
- 1286
- ISSN
- 0960-894X
1464-3405
- 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 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.
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Related Researcher
- Lee, Kyeong
- College of Pharmacy (Department of Pharmacy)