Abstract
We have developed a novel class of cdc25A inhibitors by drastic modification of the hydrophobic and hydrophilic substructures of dysidiolide. The unsaturated derivative 3b strongly inhibited cdc25A (IC50 = 7.7 microM) and caused GI arrest of HL60 cells.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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4-Butyrolactone / analogs & derivatives
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4-Butyrolactone / chemistry
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4-Butyrolactone / pharmacology
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Antineoplastic Agents / chemical synthesis
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / pharmacology*
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Cholecalciferol / analogs & derivatives*
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Cholecalciferol / pharmacology
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Enzyme Inhibitors / chemical synthesis*
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Enzyme Inhibitors / chemistry
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Enzyme Inhibitors / pharmacology
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G1 Phase / drug effects*
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HL-60 Cells
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Humans
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cdc25 Phosphatases / antagonists & inhibitors*
Substances
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Antineoplastic Agents
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Enzyme Inhibitors
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Cholecalciferol
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CDC25A protein, human
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cdc25 Phosphatases
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dysidiolide
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4-Butyrolactone