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

doi:10.1016/j.bmcl.2016.01.016

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^*

^*Corresponding author for this work

Research output: Contribution to journal › Article › peer-review

18 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 language	English
Pages (from-to)	1282-1286
Number of pages	5
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	26
Issue number	4
DOIs	https://doi.org/10.1016/j.bmcl.2016.01.016
Publication status	Published - 2016 Feb 15

Bibliographical note

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

Keywords

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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10.1016/j.bmcl.2016.01.016

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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

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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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doi = "10.1016/j.bmcl.2016.01.016",

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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

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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 - IL-6 antagonists

KW - IL-6 signaling inhibitor

KW - Oxazolidinone

KW - Rheumatoid arthritis

KW - STAT3

KW - gp130

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DO - 10.1016/j.bmcl.2016.01.016

M3 - Article

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AN - SCOPUS:84958103583

SN - 0960-894X

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SP - 1282

EP - 1286

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 4

ER -

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

Abstract

Bibliographical note

Keywords

ASJC Scopus subject areas

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