Structure-activity relationship studies of small-molecule inhibitors of Wnt response

Jianming Lu, Zhiqiang Ma, Jen Chieh Hsieh, Chih Wei Fan, Baozhi Chen, Jamie C. Longgood, Noelle S. Williams, James F. Amatruda, Lawrence Lum, Chuo Chen

Research output: Contribution to journalArticlepeer-review

113 Scopus citations


Suppression of oncogenic Wnt-mediated signaling holds promise as an anti-cancer therapeutic strategy. We previously reported a novel class of small molecules (IWR-1/2, inhibitors of Wnt response) that antagonize Wnt signaling by stabilizing the Axin destruction complex. Herein, we present the results of structure-activity relationship studies of these compounds.

Original languageEnglish (US)
Pages (from-to)3825-3827
Number of pages3
JournalBioorganic and Medicinal Chemistry Letters
Issue number14
StatePublished - Jul 15 2009


  • IWR
  • Inhibitor
  • SAR
  • Wnt

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry


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