STEROID SULFAMATE, METHOD FOR PRODUCING THE SAME AND APPLICATION THEREOF

摘要

PROBLEM TO BE SOLVED: To obtain a sulfatase inhibitor having no estrogenic active ingredient, because a compound restricting or preventing utilization of estrogenic substances is required for hormone dependent tumors.

SOLUTION: A new estratriene of formula (I) containing some sulfamoyloxy groups (m=1-5) in the molecule is provided. This compound is produced by reacting a proper steroid alcohol with sulfamoyl chloride, an n-alkyl chloride or an alkanoylsulfamoyl in the presence of a buffer solution or a base. The compound of formula (I) has high sulfatase activity and so is suitable for treating diseases reacting to sulfatase inhibition. By target high specificity of the compound in sulfatase and estrogen transfer assay, the compound labeled with a radioisotope (e.g. substituting [F18] fluorine for its F) is usable as a possible marker in tumor diagnoses.

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