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

Department of Biotechnology

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

13 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

Funding Information:
This work was supported by a grant of Basic Science Research Program through the National Research Foundation of Korea (NRF) grant funded by the Korea government (MSIP) (No. 2014R1A2A2A01005455) and Ministry of Education, Science and Technology ( 2103R1A1A2013610 ), Republic of Korea.

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.",

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note = "Funding Information: This work was supported by a grant of Basic Science Research Program through the National Research Foundation of Korea (NRF) grant funded by the Korea government (MSIP) (No. 2014R1A2A2A01005455) and Ministry of Education, Science and Technology ( 2103R1A1A2013610 ), Republic of Korea. Publisher Copyright: {\textcopyright} 2016 Elsevier Ltd. All rights reserved.",

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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

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KW - IL-6 signaling inhibitor

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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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