Synthesis, Biological Evaluation and the Rationalisation of the Inhibitory Activity of a Range of Sulfonate Derivatives of Estrone (E1) in the Design of Reversible Inhibitors of Estrone Sulfatase (ES)

ISSN: 1875-628X (Online)
ISSN: 1570-1808 (Print)


Volume 11, 10 Issues, 2014


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Synthesis, Biological Evaluation and the Rationalisation of the Inhibitory Activity of a Range of Sulfonate Derivatives of Estrone (E1) in the Design of Reversible Inhibitors of Estrone Sulfatase (ES)

Author(s): Mohsen Akbarzadeh, Timothy Cartledge and Sabbir Ahmed

Affiliation: Institute of Biomedical and Environmental Health Research (IBEHR), School of Science, Faculty of Science and Technology, University of the West of Scotland, High Street, Paisley, Renfrewshire, PA1 2BE, Scotland, UK.

Abstract

Sulfonate derivatives of estrone (E1) were designed and synthesized as potential reversible inhibitors of E1 sulfatase (ES). The results of the biochemical evaluation show the compounds to be weak inhibitors in comparison to the irreversible inhibitor E1-3-O-sulfamate, however, two compounds were found to possess good inhibitory activity.




Keywords: Breast cancer, Estrone sulfatase, Reversible inhibition, Substrate mimic, Sulfonated derivative.

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Article Details

Volume: 11
Issue Number: 8
First Page: 985
Last Page: 992
Page Count: 8
DOI: 10.2174/1570180811666140226235116
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