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, Chirag K. Patel

Journal Name: Letters in Drug Design & Discovery

Volume 11 , Issue 4 , 2014


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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.

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

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Article Details

VOLUME: 11
ISSUE: 4
Year: 2014
Page: [437 - 443]
Pages: 7
DOI: 10.2174/15701808113106660081
Price: $65

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