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

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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.

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
State	Published - 15 Feb 2016

Bibliographical note

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

Keywords

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

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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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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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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.

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KW - IL-6 signaling inhibitor

KW - Oxazolidinone

KW - Rheumatoid arthritis

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IS - 4

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

Abstract

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Keywords

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