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Synthesis and sulfatase inhibitory activities ..

Under conditions associated with reduced estrogen synthesis in humans (aromatase deficiency, placental sulfatase deficiency, fetal anencephaly), estrogen production and concentrations may be reduced by 80-90%.

Estrone sulfate partially blocked the inactivation of the enzyme by the compound, indicating that the compound inactivated sulfatase at the active site.

Synthesis and sulfatase inhibitory activities of non-steroidal estrone sulfatase ..
Photo provided by Flickr

Steroid sulfatase (STS) catalyzes the ..

Thus, (p-O-sulfamoyl)-N-alkanoyl tyramines represent a new series of non-steroidal estrone sulfatase inhibitor.
Photo provided by Flickr

However, a recent report indicated that estrone may be released during the inactivation of sulfatase by estrone-3-O-sulfamate and rendered the inhibitor to be estrogenic.

Routes of administration and dosages of commonly used estrogens Estrogen Route Dosage Natural and equine estrogens Conjugated equine estrogens Oral 0.3-2.5 mg/day Intramuscular 25 mg/day Intravenous 25 mg/day Vaginal 2-4 g/day Piperazine estrone sulfate Oral 0.625-2.5 mg/day Vaginal 2-4 g/day Estradiol Patch 0.05-0.1 mg every 3-4 days Vaginal 1-4 g/day Micronized, valerate Oral 1-2 mg/day Valerate Intramuscular 10 mg/month Cypionate Intramuscular 1-5 mg/month Synthetic estrogens Ethinylestradiol Oral 20-50 µg/day Mestranol Oral 50-100 µg/day Diethylstilbestrol Oral 1-5 mg/day Quinestrol Oral 0.1 mg/day Table 17.

Synthesis of 4-formyl estrone ..

Several research groups have reported the development of estrone sulfatase inhibitors, and estrone-3-O-sulfamate has been shown to be the most potent sulfatase inhibitor.

Thus, (p-O-sulfamoyl)-N-alkanoyl tyramines represent a new series of non-steroidal estrone sulfatase inhibitor.
Photo provided by Flickr

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Estrone sulfate analogs as estrone sulfatase inhibitors

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