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

Chirag K. Patel; Caroline P. Owen; Sabbir Ahmed

doi:10.1016/j.bmcl.2003.11.067

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

Chirag K. Patel
, Caroline P. Owen
, Sabbir Ahmed

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 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.

Original language	English
Pages (from-to)	605-609
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	14
Issue number	3
DOIs	https://doi.org/10.1016/j.bmcl.2003.11.067
Publication status	Published - 9 Feb 2004
Externally published	Yes

Keywords

physicochemical factor
biochemical evaluation
Chemistry

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10.1016/j.bmcl.2003.11.067

http://dx.doi.org/doi:10.1016/j.bmcl.2003.11.067

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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.",

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AU - Owen, Caroline P.

AU - Ahmed, Sabbir

PY - 2004/2/9

Y1 - 2004/2/9

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 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.

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 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.

KW - physicochemical factor

KW - biochemical evaluation

KW - Chemistry

UR - http://www.ncbi.nlm.nih.gov/pubmed/14741252

U2 - 10.1016/j.bmcl.2003.11.067

DO - 10.1016/j.bmcl.2003.11.067

M3 - Article

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SN - 0960-894X

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SP - 605

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JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 3

ER -

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

Abstract

Keywords

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