title: Structure-activity relationship study of a series of novel oxazolidinone derivatives as IL-6 signaling blockers.
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.
authors.affiliation: College of Phamacy, Dongguk University-Seoul, Goyang 10326, Republic of Korea; College of Life Sciences and Biotechnology, Korea University, Seoul 02841, Republic of Korea.
authors.forename: Sarbjit
authors.initials: S
authors.lastname: Singh
authors.affiliation: College of Life Sciences and Biotechnology, Korea University, Seoul 02841, Republic of Korea.
authors.forename: Veeraswamy
authors.initials: V
authors.lastname: Gajulapati
authors.affiliation: College of Life Sciences and Biotechnology, Korea University, Seoul 02841, Republic of Korea.
authors.forename: Kondaji
authors.initials: K
authors.lastname: Gajulapati
authors.affiliation: College of Life Sciences and Biotechnology, Korea University, Seoul 02841, Republic of Korea.
authors.forename: Ja-Il
authors.initials: JI
authors.lastname: Goo
authors.affiliation: College of Phamacy, The Gatholic University of Korea, Bucheon 420-743, Republic of Korea.
authors.forename: Yeon-Hwa
authors.initials: YH
authors.lastname: Park
authors.affiliation: College of Life Sciences and Biotechnology, Korea University, Seoul 02841, Republic of Korea.
authors.forename: Hwa Young
authors.initials: HY
authors.lastname: Jung
authors.affiliation: College of Life Sciences and Biotechnology, Korea University, Seoul 02841, Republic of Korea.
authors.forename: Sung Yoon
authors.initials: SY
authors.lastname: Lee
authors.affiliation: Natural Medicine Reasearch Center, Korea Research Institute of Bioscience and Biotechnology, Chungbuk 363-883, Republic of Korea.
authors.forename: Jung Ho
authors.initials: JH
authors.lastname: Choi
authors.affiliation: Natural Medicine Reasearch Center, Korea Research Institute of Bioscience and Biotechnology, Chungbuk 363-883, Republic of Korea.
authors.forename: Young Kook
authors.initials: YK
authors.lastname: Kim
authors.affiliation: College of Phamacy, Dongguk University-Seoul, Goyang 10326, Republic of Korea.
authors.forename: Kyeong
authors.initials: K
authors.lastname: Lee
authors.affiliation: College of Phamacy, The Gatholic University of Korea, Bucheon 420-743, Republic of Korea.
authors.forename: Tae-Hwe
authors.initials: TH
authors.lastname: Heo
authors.affiliation: College of Life Sciences and Biotechnology, Korea University, Seoul 02841, Republic of Korea. Electronic address: ychoi@korea.ac.kr.
authors.forename: Yongseok
authors.initials: Y
authors.lastname: Choi
mesh_terms: D001665:Binding Sites; D019086:Bridged Bicyclo Compounds, Heterocyclic / Q000737:chemistry; D018360:Crystallography, X-Ray; D056945:Hep G2 Cells; D006801:Humans; D007211:Indoles / Q000737:chemistry; D020128:Inhibitory Concentration 50; D015850:Interleukin-6 / Q000378:metabolism*; D062105:Molecular Docking Simulation; D023303:Oxazolidinones / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D017434:Protein Structure, Tertiary; D050796:STAT3 Transcription Factor / Q000235:genetics / Q000378:metabolism; D015398:Signal Transduction / Q000187:drug effects*; D013329:Structure-Activity Relationship; D000093242:Interleukin-6 Inhibitors
chemical_list: D019086:Bridged Bicyclo Compounds, Heterocyclic; D007211:Indoles; D015850:Interleukin-6; D023303:Oxazolidinones; D050796:STAT3 Transcription Factor; D000093242:Interleukin-6 Inhibitors; C103158:madindoline A
keywords: IL-6 antagonists; IL-6 signaling inhibitor; Oxazolidinone; Rheumatoid arthritis; STAT3; gp130