Novel inhibitors of the enzyme estrone sulfatase (ES)

Bioorg Med Chem Lett. 2001 Mar 26;11(6):841-4. doi: 10.1016/s0960-894x(01)00086-5.

Abstract

We report the initial results of our study into a series of simple 4-sulfamated phenyl alkyl ketones as potential inhibitors of the enzyme estrone sulfatase. The results of the study show that these compounds are potent inhibitors, possessing greater inhibitory activity than COUMATE, but weaker activity than EMATE. Furthermore, the compounds are observed to be irreversible inhibitors.

Publication types

  • Comparative Study

MeSH terms

  • Alkanes / chemical synthesis*
  • Alkanes / chemistry
  • Alkanes / pharmacology*
  • Coumarins / pharmacology
  • Enzyme Inhibitors / chemical synthesis
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / pharmacology*
  • Estrone / analogs & derivatives
  • Estrone / pharmacology
  • Inhibitory Concentration 50
  • Ketones / chemical synthesis
  • Ketones / chemistry
  • Ketones / pharmacology*
  • Mesylates / chemical synthesis*
  • Mesylates / chemistry
  • Mesylates / pharmacology
  • Sulfatases / antagonists & inhibitors*
  • Sulfatases / metabolism
  • Sulfonamides / pharmacology
  • Sulfonic Acids / chemical synthesis
  • Sulfonic Acids / chemistry
  • Sulfonic Acids / pharmacology*

Substances

  • 2-Tetradecylbutane-1,4-diol dimethanesulphonate
  • 4-methylcoumarin 7-O-sulfamate
  • Alkanes
  • Coumarins
  • Enzyme Inhibitors
  • Ketones
  • Mesylates
  • Sulfonamides
  • Sulfonic Acids
  • estrone-3-O-sulfamate
  • Estrone
  • sulfamic acid
  • Sulfatases
  • estrone sulfatase