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 a novel inhibitors of steroid sulfatase (STS). The new compounds are potent STS 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 in the enzymatic STS 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).
Authors
- dr hab. inż. Sebastian Demkowicz link open in new tab ,
- dr inż. Mateusz Daśko link open in new tab ,
- Witold Kozak link open in new tab ,
- Katarzyna Krawczyk link open in new tab ,
- prof. dr hab. inż. Dariusz Witt link open in new tab ,
- Maciej Masłyk,
- Konrad Kubiński,
- prof. dr hab. inż. Janusz Rachoń link open in new tab
Additional information
- DOI
- Digital Object Identifier link open in new tab 10.1111/cbdd.12652
- Category
- Publikacja w czasopiśmie
- Type
- artykuł w czasopiśmie wyróżnionym w JCR
- Language
- angielski
- Publication year
- 2016
