First dual aromatase-steroid sulfatase inhibitors

L.W.L. Woo, O.B. Sutcliffe, C. Bubert, A. Grasso, S.K. Chander, A. Purohit, M.J. Reed, B.V.L. Potter

Research output: Contribution to journalArticlepeer-review

74 Citations (Scopus)

Abstract

Aromatase inhibitors in clinical use block the biosynthesis of estrogens. Hydrolysis of estrone 3-sulfate by steroid sulfatase is an important additional source of tumor estrogen, and blockade of both enzymes should provide a more effective endocrine therapy. Sulfamoylated derivatives of the aromatase inhibitor YM511 inhibited sulfatase and aromatase in JEG-3 cells with respective IC50 values of 20-227 and 0.82-100 nM (cf. letrozole, 0.89 nM). One dual inhibitor was potent against both enzymes in vivo, validating the concept.
Original languageEnglish
Pages (from-to)3193-3196
Number of pages3
JournalJournal of Medicinal Chemistry
Volume46
Issue number15
DOIs
Publication statusPublished - 2003

Keywords

  • breast carcinoma
  • endocrine therapy
  • cancer research

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