abstract |
(57) [Object] To provide a pharmaceutical composition effective in treating estrogen-dependent tumors. A pharmaceutical composition comprising a pharmaceutically acceptable carrier or diluent and a compound, wherein the compound comprises a ring system and a sulfamate group of the formula: Each of R 1 and R 2 is independently selected from H, alkyl, alkenyl, cycloalkyl, and aryl; Wherein at least one of R 1 and R 2 is H; the compound is an inhibitor of an enzyme having steroid sulfatase activity (EC 3.1.6.2); the sulfamate group of the compound Is replaced with a sulfate group to form a sulfate compound, and pH7. When incubated with the steroid sulfatase enzyme (EC 3.1.6.2) at 4 and 37 ° C., it provides a K m value of less than 50 μM. |