Synthesis and In Vitro Biochemical Evaluation of a Series of Compounds as Potential Inhibitors of Estrone Sulfatase (ES) and the Role of pKa in both the Synthesis and the Inhibitory Activity of the Potential Inhibitors

Author(s): Caroline P. Owen, Mijal Patel, Chirag K Patel, Tim Cartledge, Sabbir Ahmed

Journal Name: Letters in Drug Design & Discovery

Volume 4 , Issue 6 , 2007

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We report the results of our study into a series of 3,5-dibrominated derivatives of esters of 4- [(aminosulfonyl)oxy]benzoate as potential inhibitors of estrone sulfatase (ES). The results suggest that the compounds are weak inhibitors as a result of the incorporation of the bromine atoms which reduce the stability of the compound.

Keywords: Estrone sulfatase, Inhibition, Breast cancer pKa, Dibrominated, Benzoic acid esters

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Article Details

Year: 2007
Page: [394 - 398]
Pages: 5
DOI: 10.2174/157018007781387773
Price: $65

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