2. Academic Validation
  3. Structure-activity relationship study of a series of novel oxazolidinone derivatives as IL-6 signaling blockers

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

  • Bioorg Med Chem Lett. 2016 Feb 15;26(4):1282-6. doi: 10.1016/j.bmcl.2016.01.016.
Sarbjit Singh 1,  Veeraswamy Gajulapati 2,  Kondaji Gajulapati 2,  Ja-Il Goo 2,  Yeon-Hwa Park 3,  Hwa Young Jung 2,  Sung Yoon Lee 2,  Jung Ho Choi 4,  Young Kook Kim 4,  Kyeong Lee 5,  Tae-Hwe Heo 3,  Yongseok Choi 6
Affiliations

Affiliations

  • 1 College of Phamacy, Dongguk University-Seoul, Goyang 10326, Republic of Korea; College of Life Sciences and Biotechnology, Korea University, Seoul 02841, Republic of Korea.
  • 2 College of Life Sciences and Biotechnology, Korea University, Seoul 02841, Republic of Korea.
  • 3 College of Phamacy, The Gatholic University of Korea, Bucheon 420-743, Republic of Korea.
  • 4 Natural Medicine Reasearch Center, Korea Research Institute of Bioscience and Biotechnology, Chungbuk 363-883, Republic of Korea.
  • 5 College of Phamacy, Dongguk University-Seoul, Goyang 10326, Republic of Korea.
  • 6 College of Life Sciences and Biotechnology, Korea University, Seoul 02841, Republic of Korea. Electronic address: ychoi@korea.ac.kr.
PMID: 26810262 DOI: 10.1016/j.bmcl.2016.01.016
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.

Keywords

IL-6 antagonists; IL-6 signaling inhibitor; Oxazolidinone; Rheumatoid arthritis; STAT3; gp130.

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