Letters in Drug Design & Discovery

Atta-ur-Rahman  , FRS
Honorary Life Fellow
Kings College
University of Cambridge
Cambridge
UK
Email: lddd@benthamscience.org

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Synthesis, In Vitro Activity and Rationalisation of a Series of Dialkyl Esters of 5-Aminosulfonylisophthanoate as Potential Estrone Sulfatase (ES) Inhibitors

Author(s): Sabbir Ahmed and Chirag K. Patel

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, PA1 2BE, Scotland, UK.

Keywords: Estrone sulfatase, Irreversible, Inhibition, Breast cancer, Isophthanoic acid esters, Electron density, ES inhibitor.

Graphical Abstract:


Abstract:

We consider dialkyl esters of 5-aminosulfonylisophthanoate-based compounds in our efforts to determine factors involved in determining the overall inhibitory activity against estrone sulfatase (ES). We propose that the weak inhibition observed is due to the increased electron density in the area of the phenyl ring close to the sulfamate moiety.

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Article Details

VOLUME: 11
ISSUE: 4
Page: [437 - 443]
Pages: 7
DOI: 10.2174/15701808113106660081