What is it about?
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 lM (the IC50 value of coumarin-7-O-sulfamate is 3.5 lM, used as a reference).
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Why is it important?
New steroid sulfatase inhibitors
Perspectives
New target for the treatment of breast cancer
Prof Janusz Rachon
Gdansk University of Technology
Read the Original
This page is a summary of: Synthesis and biological evaluation ofN-acylated tyramine sulfamates containing C-F bonds as steroid sulfatase inhibitors, Chemical Biology & Drug Design, February 2017, Wiley,
DOI: 10.1111/cbdd.12931.
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