Synthesis and sulfatase inhibitory activities of (E)- and (Z)-4-hydroxytamoxifen sulfamates |
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| Authors: | Chu G H Peters A Selcer K W Li P K |
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| Affiliation: | Department of Medicinal Chemistry and Pharmaceutics, Mylan School of Pharmacy, Duquesne University, Pittsburgh, PA 15282, USA. |
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| Abstract: | We report the development of (E)- and (Z)-4-hydroxytamoxifen sulfamates as estrone sulfatase inhibitors, potential therapeutic agents for the treatment of breast cancer. Both compounds competitively inhibit estrone sulfatase isolated from rat liver with apparent Ki of 35.9 microM for (E)-4-hydroxytamoxifen sulfamate and an apparent Ki of > 500 microM for the (Z) isomer. |
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