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

@article{Walter20042PhenylindoleSI,
  title={2-Phenylindole sulfamates: inhibitors of steroid sulfatase with antiproliferative activity in MCF-7 breast cancer cells},
  author={G. Walter and R Scott Liebl and Erwin von Angerer},
  journal={The Journal of Steroid Biochemistry and Molecular Biology},
  year={2004},
  volume={88},
  pages={409-420}
}
A number of 2-phenylindole sulfamates with lipophilic side chains in 1- 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 IC(50) values between 2 nM and 1 microM. A favorable position for a long side chain is the nitrogen of a carbamoyl group at C-5 of the indole when the phenyl ring carries the sulfamate function… CONTINUE READING
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