TY - JOUR
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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U2 - 10.1016/j.bmcl.2004.10.034
DO - 10.1016/j.bmcl.2004.10.034
M3 - Article
C2 - 15582411
AN - SCOPUS:9644262444
SN - 0960-894X
VL - 15
SP - 61
EP - 65
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
IS - 1
ER -