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 journalArticle

2 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

Fingerprint

Oxazolidinones
Structure-Activity Relationship
Interleukin-6
Derivatives
Inhibitory Concentration 50
Hep G2 Cells
Luciferases

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

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

In: Bioorganic and Medicinal Chemistry Letters, Vol. 26, No. 4, 15.02.2016, p. 1282-1286.

Research output: Contribution to journalArticle

Singh, S, Gajulapati, V, Gajulapati, K, Goo, JI, Park, YH, Jung, HY, Lee, SY, Choi, JH, Kim, YK, Lee, K, Heo, TH & Choi, Y 2016, 'Structure-activity relationship study of a series of novel oxazolidinone derivatives as IL-6 signaling blockers', Bioorganic and Medicinal Chemistry Letters, vol. 26, no. 4, pp. 1282-1286. https://doi.org/10.1016/j.bmcl.2016.01.016
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. / Structure-activity relationship study of a series of novel oxazolidinone derivatives as IL-6 signaling blockers. In: Bioorganic and Medicinal Chemistry Letters. 2016 ; Vol. 26, No. 4. pp. 1282-1286.
@article{8bd0d77e29824fa0ac70f8b3154834d7,
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.",
keywords = "gp130, IL-6 antagonists, IL-6 signaling inhibitor, Oxazolidinone, Rheumatoid arthritis, STAT3",
author = "Sarbjit Singh and Veeraswamy Gajulapati and Kondaji Gajulapati and Goo, {Ja Il} and Park, {Yeon Hwa} and Jung, {Hwa Young} and Lee, {Sung Yoon} and Choi, {Jung Ho} and Kim, {Young Kook} and Kyeong Lee and Heo, {Tae Hwe} and Yongseok Choi",
year = "2016",
month = "2",
day = "15",
doi = "10.1016/j.bmcl.2016.01.016",
language = "English",
volume = "26",
pages = "1282--1286",
journal = "Bioorganic and Medicinal Chemistry Letters",
issn = "0960-894X",
publisher = "Elsevier Limited",
number = "4",

}

TY - JOUR

T1 - Structure-activity relationship study of a series of novel oxazolidinone derivatives as IL-6 signaling blockers

AU - Singh, Sarbjit

AU - Gajulapati, Veeraswamy

AU - Gajulapati, Kondaji

AU - Goo, Ja Il

AU - Park, Yeon Hwa

AU - Jung, Hwa Young

AU - Lee, Sung Yoon

AU - Choi, Jung Ho

AU - Kim, Young Kook

AU - Lee, Kyeong

AU - Heo, Tae Hwe

AU - Choi, Yongseok

PY - 2016/2/15

Y1 - 2016/2/15

N2 - 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.

AB - 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.

KW - gp130

KW - IL-6 antagonists

KW - IL-6 signaling inhibitor

KW - Oxazolidinone

KW - Rheumatoid arthritis

KW - STAT3

UR - http://www.scopus.com/inward/record.url?scp=84958103583&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=84958103583&partnerID=8YFLogxK

U2 - 10.1016/j.bmcl.2016.01.016

DO - 10.1016/j.bmcl.2016.01.016

M3 - Article

C2 - 26810262

AN - SCOPUS:84958103583

VL - 26

SP - 1282

EP - 1286

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

SN - 0960-894X

IS - 4

ER -