Abstract
Some simplified adociaquinone B analogs and a series of 1,4-naphthoquinone derivatives were synthesized and tested against the three enzymes Cdc25B, MKP-1, and MKP-3. Cdc25B and MKP-1 in particular are enzymes overexpressed in human cancer cells, and they represent potential molecular targets for novel cancer chemotherapeutic treatments. A number of analogs exhibited significant inhibitory activity against these enzymes, and the bioassay data in addition to structure-activity relationships of these compounds will be discussed.
Publication types
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Research Support, N.I.H., Extramural
MeSH terms
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Cell Line, Tumor
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Cell Proliferation / drug effects
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Cyclic S-Oxides / pharmacology*
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Dual Specificity Phosphatase 1 / antagonists & inhibitors*
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Dual Specificity Phosphatase 6 / antagonists & inhibitors*
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Enzyme Inhibitors / pharmacology*
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Humans
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Magnetic Resonance Spectroscopy
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Naphthoquinones / pharmacology*
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Spectrometry, Mass, Electrospray Ionization
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cdc25 Phosphatases / antagonists & inhibitors*
Substances
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Cyclic S-Oxides
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Enzyme Inhibitors
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Naphthoquinones
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adociaquinone B
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Dual Specificity Phosphatase 1
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Dual Specificity Phosphatase 6
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cdc25 Phosphatases