Novel inhibitors of the enzyme estrone sulfatase (ES)

We report the initial results of our study into a series of simple 4-sulfamated phenyl alkyl ketones as potential inhibitors of the enzyme estrone sulfatase. The results of the study show that these compounds are potent inhibitors, possessing greater inhibitory activity than COUMATE, but weaker acti...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2001-03, Vol.11 (6), p.841-844
Main Authors: Ahmed, Sabbir, James, Karen, Owen, Caroline P, Patel, Chirag K, Patel, Mijal
Format: Article
Language:English
Subjects:
Alkanes - chemical synthesis
Alkanes - chemistry
Alkanes - pharmacology
Biological and medical sciences
Coumarins - pharmacology
Enzyme Inhibitors - chemical synthesis
Enzyme Inhibitors - chemistry
Enzyme Inhibitors - pharmacology
Estrone - analogs & derivatives
Estrone - pharmacology
Hormones. Endocrine system
Inhibitory Concentration 50
Ketones - chemical synthesis
Ketones - chemistry
Ketones - pharmacology
Medical sciences
Mesylates - chemical synthesis
Mesylates - chemistry
Mesylates - pharmacology
Pharmacology. Drug treatments
Sulfatases - antagonists & inhibitors
Sulfatases - metabolism
Sulfonamides - pharmacology
Sulfonic Acids - chemical synthesis
Sulfonic Acids - chemistry
Sulfonic Acids - pharmacology
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Summary:We report the initial results of our study into a series of simple 4-sulfamated phenyl alkyl ketones as potential inhibitors of the enzyme estrone sulfatase. The results of the study show that these compounds are potent inhibitors, possessing greater inhibitory activity than COUMATE, but weaker activity than EMATE. Furthermore, the compounds are observed to be irreversible inhibitors. The synthesis and biochemical evaluation of novel inhibitors of estrone sulfatase is reported.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(01)00086-5