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

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3 Citations (Scopus)

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 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
Volume26
Issue number4
DOIs
Publication statusPublished - 2016 Feb 15

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Keywords

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

ASJC Scopus subject areas

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

Cite this

Singh, S., Gajulapati, V., Gajulapati, K., Goo, J. I., Park, Y. H., Jung, H. Y., Lee, S. Y., Choi, J. H., Kim, Y. K., Lee, K., Heo, T. H., & Choi, Y. (2016). Structure-activity relationship study of a series of novel oxazolidinone derivatives as IL-6 signaling blockers. Bioorganic and Medicinal Chemistry Letters, 26(4), 1282-1286. https://doi.org/10.1016/j.bmcl.2016.01.016