Abstract
In our search for potent inhibitors of the enzyme estrone sulfatase (ES), we have undertaken the synthesis and biochemical evaluation of a range of esters of 4-[(aminosulfonyl)oxy] benzoic acid. The results of the study show that the synthesised compounds possess potent inhibitory activity, indeed the cyclooctyl derivative was found to be more potent than 667-COUMATE, which is currently undergoing clinical trials.
MeSH terms
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Antineoplastic Agents / chemical synthesis
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Antineoplastic Agents / pharmacology
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Benzoic Acid / chemical synthesis
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Benzoic Acid / chemistry
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Benzoic Acid / pharmacology*
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Coumarins / pharmacology
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Enzyme Inhibitors / chemical synthesis
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Enzyme Inhibitors / pharmacology*
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Esters
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Inhibitory Concentration 50
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Structure-Activity Relationship
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Sulfatases / antagonists & inhibitors*
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Sulfonamides / pharmacology
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Sulfonic Acids
Substances
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Antineoplastic Agents
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Coumarins
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Enzyme Inhibitors
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Esters
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Sulfonamides
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Sulfonic Acids
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irosustat
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Benzoic Acid
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sulfamic acid
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Sulfatases
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estrone sulfatase