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, Sabbir Ahmed.

Journal Name:Letters in Drug Design & Discovery

Volume 11 , Issue 8 , 2014

Graphical Abstract:


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: 8
Year: 2014
Page: [985 - 992]
Pages: 8
DOI: 10.2174/1570180811666140226235116
Price: $58