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

Sabbir Ahmed; Karen James; Caroline P. Owen

doi:10.1016/S0960-894X(02)00383-9

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

Sabbir Ahmed
, Karen James
, Caroline P. Owen

Research output: Contribution to journal › Article › peer-review

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 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.

Original language	English
Pages (from-to)	2391-2394
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	12
Issue number	17
DOIs	https://doi.org/10.1016/S0960-894X(02)00383-9
Publication status	Published - 2 Sept 2002

Keywords

aromatase inhibitors
Chemistry

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10.1016/S0960-894X(02)00383-9

http://dx.doi.org/10.1016/S0960-894X(02)00383-9

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

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 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.",

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AU - Ahmed, Sabbir

AU - James, Karen

AU - Owen, Caroline P.

PY - 2002/9/2

Y1 - 2002/9/2

N2 - 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.

AB - 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.

KW - aromatase inhibitors

KW - Chemistry

UR - http://www.ncbi.nlm.nih.gov/pubmed/12161140

U2 - 10.1016/S0960-894X(02)00383-9

DO - 10.1016/S0960-894X(02)00383-9

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SP - 2391

EP - 2394

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 17

ER -

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

Abstract

Keywords

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