Abstract
An efficient synthesis of dialkylsubstituted maleic anhydrides 1a-j is described. The inhibitory potential of these original anhydride derivatives was tested toward the three human isoforms A, B and C of dual specific phosphatases Cdc25. A micromolar range inhibition of Cdc25s was observed with the maleic anhydrides bearing simple alkyl side chains longer than C(9), to reach the optimal activity with a C(17) chain length.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Alkaline Phosphatase / antagonists & inhibitors
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Alkaline Phosphatase / chemistry
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Animals
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Horses
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Humans
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Isoenzymes / antagonists & inhibitors
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Isoenzymes / chemistry
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Liver / enzymology
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Maleic Anhydrides / chemical synthesis*
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Maleic Anhydrides / chemistry
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Nitrophenols / chemistry
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Organophosphorus Compounds / chemistry
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Structure-Activity Relationship
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cdc25 Phosphatases / antagonists & inhibitors*
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cdc25 Phosphatases / chemistry
Substances
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Isoenzymes
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Maleic Anhydrides
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Nitrophenols
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Organophosphorus Compounds
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nitrophenylphosphate
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Alkaline Phosphatase
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cdc25 Phosphatases