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2-phenylindole sulfamates: inhibitors of steroid sulfatase with antiproliferative activity in MCF-7 breast cancer cells

Walter, Georg ; Liebl, Renate ; Angerer, Erwin von



Abstract

A number of 2-phenylindole sulfamates with lipophilic side chains in I - or 5-position of the indole were synthesized and evaluated as steroid sulfatase (estrone sulfatase) inhibitors. Most of the new sulfamates inhibited the enzymatic hydrolysis of estrone sulfate in MDA-MB 231 breast cancer cells with IC50 values between 2 nM and I muM. A favorable position for a long side chain is the nitrogen ...

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