Hybrid dual aromatase-steroid sulfatase inhibitors with exquisite picomolar inhibitory activity

L. W. Lawrence Woo, Christian Bubert, Atul Purohit, Barry V. L. Potter

Research output: Contribution to journalArticlepeer-review

37 Citations (SciVal)


Single agents against multiple drug targets are highly topical. Hormone-dependent breast cancer (HDBC) may be more effectively treated by dual inhibition of aromatase and steroid sulfatase (STS), and several dual aromatase-sulfatase inhibitors (DASIs) have been recently reported. The best compounds from two leading classes of DASI, 3 and 9, are low nanomolar inhibitors. In search of a novel class of DASI, core motifs of two leading classes were combined to give a series of hybrid structures, with several compounds showing markedly improved dual inhibitory activities in the picomolar range in JEG-3 cells. Thus, DASIs 14 (IC50: aromatase, 15 pM; STS, 830 pM) and 15 (IC50: aromatase, 18 pM; STS, 130 pM) are the first examples of an exceptional new class of highly potent dual inhibitor that should encourage further development toward multitargeted therapeutic intervention in HDBC.
Original languageEnglish
Pages (from-to)243-247
JournalACS Medicinal Chemistry Letters
Issue number3
Publication statusPublished - Mar 2011


  • sulfatase
  • aromatase
  • hybrid
  • dual inhibitors
  • cancer


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