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