Steroid sulfatase inhibitors and methods for making and using th

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Cyclopentanohydrophenanthrene ring system doai

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514182, 552522, 552611, A61K 3156, C07J 300, C07J 4100

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active

058801154

ABSTRACT:
Sulfatase inhibitor compounds having the formula: ##STR1## wherein X, Y, R.sub.1, R.sub.2 and R.sub.3 are as defined in the specification. The compounds are useful in the treatment of estrogen dependent illnesses. Methods for synthesizing these compounds are also disclosed.

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Duncan et al., "Inhibition of Estrone Sulfatase Activity by Estrone-3-methylthiophosphonate: A Potential Therapeutic Agent in Breast Cancer", Cancer Res., vol. 53, pp. 298-302 (Jan. 15, 1993).
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Howarth et al., "Estrone Sulfamates: Potent Inhibitors of Estrone Sulfatase with Therapeutic Potential", J. Med. Chem., vol. 37, pp. 219-221 (1994).
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Li et al., "Estrone sulfate analogs as estrone sulfatase inhibitors", Steroids, vol. 60, pp. 299-306 (1995).
Selcer et al., "Inhibition of Placental Estrone Sulfatase Activity and MCF-7 Breast Cancer Cell Proliferation by Estrone-3-amino Derivatives", J. Steriod Biochem. Molec. Biol., vol. 59, No. 1, pp. 83-91 (1996).

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