Inhibition of estrone sulfatase (ES) by derivatives of 4-[(aminosulfonyl)oxy] benzoic acid

In our search for potent inhibitors of the enzyme estrone sulfatase (ES), we have undertaken the synthesis and biochemical evaluation of a range of straight chain alkyl esters of 4-[(aminosulfonyl)oxy] benzoic acid. The results of the study show that the synthesised compounds possess greater inhibit...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2002-09, Vol.12 (17), p.2391-2394
Main Authors: Ahmed, Sabbir, James, Karen, Owen, Caroline P
Format: Article
Language:English
Subjects:
Antineoplastic agents
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - pharmacology
Benzoates - chemical synthesis
Benzoates - pharmacology
Biological and medical sciences
General aspects
Humans
Hydrophobic and Hydrophilic Interactions
Inhibitory Concentration 50
Medical sciences
Pharmacology. Drug treatments
Structure-Activity Relationship
Sulfatases - antagonists & inhibitors
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Summary:In our search for potent inhibitors of the enzyme estrone sulfatase (ES), we have undertaken the synthesis and biochemical evaluation of a range of straight chain alkyl esters of 4-[(aminosulfonyl)oxy] benzoic acid. The results of the study show that the synthesised compounds possess greater inhibitory activity when compared to COUMATE, although they were all found to possess lower inhibitory activity with respect to EMATE. Furthermore, the data suggest a strong correlation between logP and IC 50 and therefore adds further support to our previous report where we suggested a link between inhibitory activity and hydrophobicity. The inhibition of estrone sulfatase is investigated using esters of 4-aminosulfonated derivatives of benzoic acid.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(02)00383-9