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N,N-Dialkylated derivatives of the steroid sulphatase inhibitor, oestrone 3-O-sulphamate (EMATE) are weak reversible inhibitors of the enzyme. N-Acetylated-EMATE (8), but not the benzoyl derivative, inhibits the enzyme irreversibly, albeit less potently than EMATE and will allow hitherto difficult radiolabelling on the sulphamate group to facilitate investigation of the enzyme inactivation mechanism.

Original publication

DOI

10.1016/S0960-894X(97)10167-6

Type

Journal article

Journal

Bioorganic and Medicinal Chemistry Letters

Publication Date

16/12/1997

Volume

7

Pages

3075 - 3080