Synthesis and In Vitro Biochemical Evaluation of a Series of Cycloalkyl Esters of 4-Sulfamoylated Benzoic Acid as Inhibitors of Estrone Sulfatase (ES)

, Caroline P. Owen; , Chirag K. Patel; , Tim Cartledge; , Sabbir Ahmed

Synthesis and In Vitro Biochemical Evaluation of a Series of Cycloalkyl Esters of 4-Sulfamoylated Benzoic Acid as Inhibitors of Estrone Sulfatase (ES)

Author(s): Caroline P. Owen, Chirag K. Patel, Tim Cartledge, Sabbir Ahmed

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Journal Name: Letters in Drug Design & Discovery

Volume 4 , Issue 6 , 2007

DOI : 10.2174/157018007781387845

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Abstract:

We report the results of the synthesis and biochemical evaluation of esters of 4-[(aminosulfonyl)oxy]benzoate as potential inhibitors of estrone sulfatase (ES). Modelling the compounds shows that steric interaction between the inhibitor and the active site is a major factor responsible for the weak inhibitory activity observed within the synthesised compounds.

Keywords: Estrone sulfatase, Synthesis, Evaluation, Cycloalkyl esters, Breast cancer, Inhibition

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Letters in Drug Design & Discovery

Title: Synthesis and In Vitro Biochemical Evaluation of a Series of Cycloalkyl Esters of 4-Sulfamoylated Benzoic Acid as Inhibitors of Estrone Sulfatase (ES)

VOLUME: 4 ISSUE: 6

Author(s): Caroline P. Owen, Chirag K. Patel, Tim Cartledge and Sabbir Ahmed

Affiliation:Department of Pharmacy,School of Pharmacy and Chemistry, Kingston University, Penrhyn Road,Kingston upon Thames, Surrey, KT1 2EE, UK.

Keywords:Estrone sulfatase, Synthesis, Evaluation, Cycloalkyl esters, Breast cancer, Inhibition

Abstract: We report the results of the synthesis and biochemical evaluation of esters of 4-[(aminosulfonyl)oxy]benzoate as potential inhibitors of estrone sulfatase (ES). Modelling the compounds shows that steric interaction between the inhibitor and the active site is a major factor responsible for the weak inhibitory activity observed within the synthesised compounds.

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Caroline P. Owen, Chirag K. Patel, Tim Cartledge and Sabbir Ahmed, “ Synthesis and In Vitro Biochemical Evaluation of a Series of Cycloalkyl Esters of 4-Sulfamoylated Benzoic Acid as Inhibitors of Estrone Sulfatase (ES)”, Letters in Drug Design & Discovery (2007) 4: 399. https://doi.org/10.2174/157018007781387845

DOI https://doi.org/10.2174/157018007781387845	Print ISSN 1570-1808
Publisher Name Bentham Science Publisher	Online ISSN 1875-628X

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Article Details

VOLUME: 4
ISSUE: 6
Year: 2007

Page: [399 - 403]
Pages: 5
DOI: 10.2174/157018007781387845
Price: $65

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