estran - sulphamatederivaten as steroid sulfatase inhibitory compounds

摘要

There is provided a purified compound of the formula CHEM wherein R1 and R2 are H; and wherein the group Polycycle is a residue of an oestrogen wherein the compound is an inhibitor of an enzyme having steroid sulphatase activity (E.C.3.1.6.2); wherein if the sulphamate group on the compound were to be replaced with a sulphate group to form a sulphate compound and incubated with a steroid sulphatase enzyme (E.C.3.1.6.2) at a pH 7.4 and 37 DEG C it would provide a Km value of less than 50 mu M. IMAGE