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

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.