Abstract
A series of benzotriazole phenyldifluoromethylphosphonic acids were found to be potent PTP-1B inhibitors. Molecular modeling on the X-ray crystal structure of the lead structure led to the design of potent PTP-1B inhibitors that show moderate selectivity against TC-PTP, a very closely related protein tyrosine phosphatase.
MeSH terms
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Animals
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Cell Line
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Cell Survival / drug effects
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Crystallography, X-Ray
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Drug Design
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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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Insecta
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Mice
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Mice, Knockout
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Models, Molecular
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Molecular Structure
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Organophosphorus Compounds / chemical synthesis
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Organophosphorus Compounds / chemistry*
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Organophosphorus Compounds / pharmacology*
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Protein Tyrosine Phosphatase, Non-Receptor Type 1
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Protein Tyrosine Phosphatases / antagonists & inhibitors*
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Structure-Activity Relationship
Substances
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Enzyme Inhibitors
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Organophosphorus Compounds
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methylphosphonic acid
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Protein Tyrosine Phosphatase, Non-Receptor Type 1
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Protein Tyrosine Phosphatases
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Ptpn1 protein, mouse