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

Journal Name: Letters in Drug Design & Discovery

Volume 4 , Issue 6 , 2007

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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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Article Details

Year: 2007
Page: [399 - 403]
Pages: 5
DOI: 10.2174/157018007781387845
Price: $65

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