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)

Title: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)

Volume: 11 Issue: 8

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

Affiliation:

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

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.

Cite this article as:

Akbarzadeh Mohsen, Cartledge Timothy and Ahmed Sabbir, 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), Letters in Drug Design & Discovery 2014; 11 (8) . https://dx.doi.org/10.2174/1570180811666140226235116

DOI https://dx.doi.org/10.2174/1570180811666140226235116	Print ISSN 1570-1808
Publisher Name Bentham Science Publisher	Online ISSN 1875-628X