Synthesis, In Vitro Activity and Rationalisation of a Series of Dialkyl Esters of 5-Aminosulfonylisophthanoate as Potential Estrone Sulfatase (ES) Inhibitors
Letters in Drug Design & Discovery,
Sabbir Ahmed and Chirag K. PatelAffiliation:
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.
AbstractWe 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.
Estrone sulfatase, Irreversible, Inhibition, Breast cancer, Isophthanoic acid esters, Electron density, ES inhibitor.
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