Synthesis and In Vitro Biochemical Evaluation of a Series of Alkyl 6- Aminosulfonyl Naphthanoates as Potential Inhibitors of Human Placental Estrone Sulfatase (ES)

Author(s): Chirag K. Patel, Sabbir Ahmed

Journal Name: Letters in Drug Design & Discovery

Volume 8 , Issue 1 , 2011

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We report the tentative initial results of our on-going search for potent inhibitors of estrone sulfatase (ES), here we report a series of alkyl 6-aminosulfonyl naphthanoate-based compounds as potential inhibitors. The results suggest that the compounds are weak inhibitors in comparison to the standard compound used within the current study.

Keywords: Estrone sulfatase, Inhibition, Irreversible, Breast cancer, Naphthanoic acid esters, aromatase, AR, estrone, estradiol, EMATE, EPSRC Mass Spectrometry, temperature, Melting points, DMA, TRITONX, TLC, 1HNMR, clogP, Benzoates, Non-Sulfamoylated Derivative, COUMATE, inhibitors, alkyl chain, substrate, transition-state, hydrophobicity, IC50

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Article Details

Year: 2011
Page: [26 - 31]
Pages: 6
DOI: 10.2174/157018011793663967

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