Journal
CHEMICAL BIOLOGY & DRUG DESIGN
Volume 87, Issue 2, Pages 233-238Publisher
WILEY
DOI: 10.1111/cbdd.12652
Keywords
breast cancer; coumarin; steroid sulfatase; steroid sulfatase inhibitors; sulfamates
Funding
- National Science Centre (Poland) [2011/03/D/NZ7/03985]
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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 mu M (the IC50 value of coumarin-7-O-sulfamate is 3.5 mu M, used as a reference).
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