Synthesis of the naphthalene-derived inhibitors against Cdc25A dual-specificity protein phosphatase and their biological activity

Akiko Shimbashi; Ayako Tsuchiya; Masaya Imoto; Shigeru Nishiyama

doi:10.1016/j.bmcl.2004.10.034

Synthesis of the naphthalene-derived inhibitors against Cdc25A dual-specificity protein phosphatase and their biological activity

Akiko Shimbashi, Ayako Tsuchiya, Masaya Imoto, Shigeru Nishiyama

Department of Biosciences and Informatics

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

5 Citations (Scopus)

Abstract

The synthesis naphthoquinones exhibited stronger activity than the pyranonaphthoquinone-type compound having moderate inhibitory activity against Cdc25A protein phosphatase. The novel naphthalene-type analogues 14 and 18 and the naphthoquinone-type analogues, 8, 9, 15, 16, 19, 21, 22, and 23-28 have been synthesized, and their in vitro Cdc25A phosphatase-inhibitory activity was examined. In assessment of the inhibitory activity, it was revealed that the naphthoquinone core is contributed to the activity, rather than the alkyl side chain.

Original language	English
Pages (from-to)	61-65
Number of pages	5
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	15
Issue number	1
DOIs	https://doi.org/10.1016/j.bmcl.2004.10.034
Publication status	Published - 2005 Jan 3

Keywords

Biological activity
Cdc25A phosphatase inhibitor
Cell cycle regulation
Dual-specificity phosphatase
Naphthoquinone

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

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title = "Synthesis of the naphthalene-derived inhibitors against Cdc25A dual-specificity protein phosphatase and their biological activity",

abstract = "The synthesis naphthoquinones exhibited stronger activity than the pyranonaphthoquinone-type compound having moderate inhibitory activity against Cdc25A protein phosphatase. The novel naphthalene-type analogues 14 and 18 and the naphthoquinone-type analogues, 8, 9, 15, 16, 19, 21, 22, and 23-28 have been synthesized, and their in vitro Cdc25A phosphatase-inhibitory activity was examined. In assessment of the inhibitory activity, it was revealed that the naphthoquinone core is contributed to the activity, rather than the alkyl side chain.",

keywords = "Biological activity, Cdc25A phosphatase inhibitor, Cell cycle regulation, Dual-specificity phosphatase, Naphthoquinone",

author = "Akiko Shimbashi and Ayako Tsuchiya and Masaya Imoto and Shigeru Nishiyama",

note = "Funding Information: This work was supported by Grant-in-Aid for the 21st Century COE program {\textquoteleft}Keio Life Conjugated Chemistry,{\textquoteright} as well as Scientific Research C from the Ministry of Education, Culture, Sports, Science, and Technology, Japan. A.S. was financially supported by the same COE program.",

year = "2005",

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doi = "10.1016/j.bmcl.2004.10.034",

language = "English",

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journal = "Bioorganic and Medicinal Chemistry Letters",

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T1 - Synthesis of the naphthalene-derived inhibitors against Cdc25A dual-specificity protein phosphatase and their biological activity

AU - Shimbashi, Akiko

AU - Tsuchiya, Ayako

AU - Imoto, Masaya

AU - Nishiyama, Shigeru

N1 - Funding Information: This work was supported by Grant-in-Aid for the 21st Century COE program ‘Keio Life Conjugated Chemistry,’ as well as Scientific Research C from the Ministry of Education, Culture, Sports, Science, and Technology, Japan. A.S. was financially supported by the same COE program.

PY - 2005/1/3

Y1 - 2005/1/3

N2 - The synthesis naphthoquinones exhibited stronger activity than the pyranonaphthoquinone-type compound having moderate inhibitory activity against Cdc25A protein phosphatase. The novel naphthalene-type analogues 14 and 18 and the naphthoquinone-type analogues, 8, 9, 15, 16, 19, 21, 22, and 23-28 have been synthesized, and their in vitro Cdc25A phosphatase-inhibitory activity was examined. In assessment of the inhibitory activity, it was revealed that the naphthoquinone core is contributed to the activity, rather than the alkyl side chain.

AB - The synthesis naphthoquinones exhibited stronger activity than the pyranonaphthoquinone-type compound having moderate inhibitory activity against Cdc25A protein phosphatase. The novel naphthalene-type analogues 14 and 18 and the naphthoquinone-type analogues, 8, 9, 15, 16, 19, 21, 22, and 23-28 have been synthesized, and their in vitro Cdc25A phosphatase-inhibitory activity was examined. In assessment of the inhibitory activity, it was revealed that the naphthoquinone core is contributed to the activity, rather than the alkyl side chain.

KW - Biological activity

KW - Cdc25A phosphatase inhibitor

KW - Cell cycle regulation

KW - Dual-specificity phosphatase

KW - Naphthoquinone

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Synthesis of the naphthalene-derived inhibitors against Cdc25A dual-specificity protein phosphatase and their biological activity

Abstract

Keywords

ASJC Scopus subject areas

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