Synthesis and sulfatase inhibitory activities of (E)- and (Z)-4-hydroxytamoxifen sulfamates.

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 Ki of 35.9 microM for (E)-4-hydroxytamoxifen sulfamate and an apparent Ki of > 500 microM for the (Z) isomer.
AuthorsG H Chu, A Peters, K W Selcer, P K Li
JournalBioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 9 Issue 2 Pg. 141-4 (Jan 18 1999) ISSN: 0960-894X [Print] ENGLAND
PMID10021916 (Publication Type: Journal Article)
Chemical References
  • Estrogen Antagonists
  • Tamoxifen
  • afimoxifene
  • Toluene
  • Sulfatases
  • estrone sulfatase
  • Animals
  • Estrogen Antagonists (chemical synthesis, pharmacology)
  • Microsomes, Liver (drug effects)
  • Rats
  • Sulfatases (antagonists & inhibitors)
  • Tamoxifen (analogs & derivatives, chemical synthesis, pharmacology)
  • Toluene (pharmacology)

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