A new NF-κB inhibitor based on the amino-epoxyquinol core of DHMEQ

Tsuyoshi Saitoh; Chika Shimada; Masatoshi Takeiri; Mitsuhiro Shiino; Shigeru Ohba; Rika Obata; Yuichi Ishikawa; Kazuo Umezawa; Shigeru Nishiyama

doi:10.1016/j.bmcl.2010.08.036

A new NF-κB inhibitor based on the amino-epoxyquinol core of DHMEQ

Tsuyoshi Saitoh, Chika Shimada, Masatoshi Takeiri, Mitsuhiro Shiino, Shigeru Ohba, Rika Obata, Yuichi Ishikawa, Kazuo Umezawa, Shigeru Nishiyama

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

8 Citations (Scopus)

Abstract

The amino-epoxyquinols 6a and 6b were synthesized as soluble derivatives of an NF-κB inhibitor DHMEQ (1). In spite of the opposite configuration from 1, 6b rather than 6a affected the deactivation of NF-κB, based on NO secretion and MALDI-TOF MS analysis. It was indicated that 6b inhibited the activation by different manner from that of 1.

Original language	English
Pages (from-to)	5638-5642
Number of pages	5
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	20
Issue number	19
DOIs	https://doi.org/10.1016/j.bmcl.2010.08.036
Publication status	Published - 2010 Oct 1
Externally published	Yes

Keywords

DHMEQ
Epoxyquinol derivatives
NF-κB inhibitor

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.2010.08.036

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title = "A new NF-κB inhibitor based on the amino-epoxyquinol core of DHMEQ",

abstract = "The amino-epoxyquinols 6a and 6b were synthesized as soluble derivatives of an NF-κB inhibitor DHMEQ (1). In spite of the opposite configuration from 1, 6b rather than 6a affected the deactivation of NF-κB, based on NO secretion and MALDI-TOF MS analysis. It was indicated that 6b inhibited the activation by different manner from that of 1.",

keywords = "DHMEQ, Epoxyquinol derivatives, NF-κB inhibitor",

author = "Tsuyoshi Saitoh and Chika Shimada and Masatoshi Takeiri and Mitsuhiro Shiino and Shigeru Ohba and Rika Obata and Yuichi Ishikawa and Kazuo Umezawa and Shigeru Nishiyama",

note = "Funding Information: This work was supported by the High-Tech Research Center Project for Private Universities Matching Fund (2006–2011) from MEXT, The Science Research Promotion Fund from The Promotion and Mutual Aid Corporation for Private Schools of Japan, and the program Promotion of Fundamental Studies in Health Sciences of the National Institute of Biomedical Innovation (NIBIO), 2006–2011. T.S. was indebted to Global COE Program {\textquoteleft}Center for Human Metabolomic Systems Biology{\textquoteright} from MEXT.",

year = "2010",

month = oct,

day = "1",

doi = "10.1016/j.bmcl.2010.08.036",

language = "English",

volume = "20",

pages = "5638--5642",

journal = "Bioorganic and Medicinal Chemistry Letters",

issn = "0960-894X",

publisher = "Elsevier Limited",

number = "19",

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TY - JOUR

T1 - A new NF-κB inhibitor based on the amino-epoxyquinol core of DHMEQ

AU - Saitoh, Tsuyoshi

AU - Shimada, Chika

AU - Takeiri, Masatoshi

AU - Shiino, Mitsuhiro

AU - Ohba, Shigeru

AU - Obata, Rika

AU - Ishikawa, Yuichi

AU - Umezawa, Kazuo

AU - Nishiyama, Shigeru

N1 - Funding Information: This work was supported by the High-Tech Research Center Project for Private Universities Matching Fund (2006–2011) from MEXT, The Science Research Promotion Fund from The Promotion and Mutual Aid Corporation for Private Schools of Japan, and the program Promotion of Fundamental Studies in Health Sciences of the National Institute of Biomedical Innovation (NIBIO), 2006–2011. T.S. was indebted to Global COE Program ‘Center for Human Metabolomic Systems Biology’ from MEXT.

PY - 2010/10/1

Y1 - 2010/10/1

N2 - The amino-epoxyquinols 6a and 6b were synthesized as soluble derivatives of an NF-κB inhibitor DHMEQ (1). In spite of the opposite configuration from 1, 6b rather than 6a affected the deactivation of NF-κB, based on NO secretion and MALDI-TOF MS analysis. It was indicated that 6b inhibited the activation by different manner from that of 1.

AB - The amino-epoxyquinols 6a and 6b were synthesized as soluble derivatives of an NF-κB inhibitor DHMEQ (1). In spite of the opposite configuration from 1, 6b rather than 6a affected the deactivation of NF-κB, based on NO secretion and MALDI-TOF MS analysis. It was indicated that 6b inhibited the activation by different manner from that of 1.

KW - DHMEQ

KW - Epoxyquinol derivatives

KW - NF-κB inhibitor

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U2 - 10.1016/j.bmcl.2010.08.036

DO - 10.1016/j.bmcl.2010.08.036

M3 - Article

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AN - SCOPUS:77957596614

SN - 0960-894X

VL - 20

SP - 5638

EP - 5642

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 19

ER -

A new NF-κB inhibitor based on the amino-epoxyquinol core of DHMEQ

Abstract

Keywords

ASJC Scopus subject areas

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