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

Sarbjit Singh, Veeraswamy Gajulapati, Kondaji Gajulapati, Ja Il Goo, Yeon Hwa Park, Hwa Young Jung, Sung Yoon Lee, Jung Ho Choi, Young Kook Kim, Kyeong Lee, Tae Hwe Heo, Yongseok Choi

Research output: Contribution to journalArticlepeer-review

15 Citations (Scopus)


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.

Original languageEnglish
Pages (from-to)1282-1286
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Issue number4
Publication statusPublished - 2016 Feb 15

Bibliographical note

Funding Information:
This work was supported by a grant of Basic Science Research Program through the National Research Foundation of Korea (NRF) grant funded by the Korea government (MSIP) (No. 2014R1A2A2A01005455) and Ministry of Education, Science and Technology ( 2103R1A1A2013610 ), Republic of Korea.

Publisher Copyright:
© 2016 Elsevier Ltd. All rights reserved.


  • IL-6 antagonists
  • IL-6 signaling inhibitor
  • Oxazolidinone
  • Rheumatoid arthritis
  • STAT3
  • gp130

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry


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