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Letters in Drug Design & Discovery


ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

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

Volume 11, Issue 4, 2014

Page: [437 - 443] Pages: 7

DOI: 10.2174/15701808113106660081

Price: $65


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.

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

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