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Bioorganic & medicinal chemistry

Sulfamoyloxy-substituted 2-phenylindoles: antiestrogen-based inhibitors of the steroid sulfatase in human breast cancer cells

T Golob, R Liebl, E von Angerer

文献索引:Golob, Thomas; Liebl, Renate; Von Angerer, Erwin Bioorganic and Medicinal Chemistry, 2002 , vol. 10, # 12 p. 3941 - 3953

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被引用次数: 48

摘要

Estrone sulfate (E1S) is an endogenous prodrug that delivers estrone and, subsequently, estradiol to the target cells following the hydrolysis by the enzyme estrone sulfatase which is active in various tissues including hormone dependent breast cancer cells. Blockade of this enzyme should reduce the estrogen level in breast cancer cells and prevent hormonal growth stimulation. Sulfamates of a variety of phenolic compounds have been shown to be ...