Synthesis and Sulfatase Inhibitory Activities of (E)- and (Z)-4-Hydroxytamoxifen Sulfamates

DOI: 10.1016/S0960-894X(98)00707-0

Source and publish data:

Bioorganic and medicinal chemistry letters p. 141 - 144 (1999)

Update date:2022-08-03

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Authors:

Chu, Guo-Hua

Peters, Amy

Selcer, Kyle W.

Li, Pui-Kai

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Article abstract of DOI:10.1016/S0960-894X(98)00707-0

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 K_i of 35.9 μM for (E)-4-hydroxytamoxifen sulfamate and an apparent K_i of >500 μM for the (Z) isomer.

Full text of DOI:10.1016/S0960-894X(98)00707-0

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