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Estrogen sulfamate derivatives were the first irreversible active-site-directed inhibitors of steroid sulfatase (STS), an emerging drug target for endocrine therapy of hormone dependent diseases that catalyzes inter alia the hydrolysis of estrone sulfate to estrone. In recent years this has stimulated clinical investigation of the estradiol derivative both as an oral prodrug and its currently ongoing exploration in endometriosis. 2-Substituted steroid sulfamate derivatives show considerable potential as multi-targeting agents for hormone-independent disease, but are also potent STS inhibitors. The steroidal template has spawned nonsteroidal STS inhibitors one of which, Irosustat, has been evaluated clinically in breast cancer, endometrial cancer and prostate cancer and there is potential for innovative dual-targeting approaches. This review surveys the role of estrogen sulfamates, their analogues and current status.

Original publication




Journal article


J Steroid Biochem Mol Biol

Publication Date





160 - 169


Cancer, Endocrine Therapy, Inhibitor, Sulfamates, Sulfatase, Synthesis, Animals, Coumarins, Enzyme Inhibitors, Estradiol, Estrogens, Estrone, Humans, Models, Molecular, Steryl-Sulfatase, Sulfonamides