Chemical Biology & Drug Design 2016-02-01

Synthesis and Biological Evaluation of Fluorinated 3-Phenylcoumarin-7-O-Sulfamate Derivatives as Steroid Sulfatase Inhibitors.

Sebastian Demkowicz, Mateusz Daśko, Witold Kozak, Katarzyna Krawczyk, Dariusz Witt, Maciej Masłyk, Konrad Kubiński, Janusz Rachon

Index: Chem. Biol. Drug Des. 87 , 233-8, (2016)

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Abstract

In the present work, we report the initial results of our study on a series of 3-phenylcoumarin sulfamate-based compounds containing C-F bonds as novel inhibitors of steroid sulfatase. The new compounds are potent steroid sulfatase inhibitors, possessing more than 10 times higher inhibitory potency than coumarin-7-O-sulfamate. In the course of our investigation, compounds 2b and 2c demonstrated the highest inhibitory effect on the enzymatic steroid sulfatase assay; both had IC50 values of 0.27 μm (the IC50 value of coumarin-7-O-sulfamate is 3.5 μm, used as a reference). © 2015 John Wiley & Sons A/S.