Synthesis and evaluation of (+)-decursin derivatives as inhibitors of the Wnt/β-catenin pathway

Jee Hyun Lee, Min Ah Kim, Seoyoung Park, Soo Hyun Cho, Eunju Yun, Yu Seok O, Jiseon Kim, Ja Il Goo, Mi Young Yun, Yongseok Choi, Sangtaek Oh, Gyu Yong Song

Research output: Contribution to journalArticlepeer-review

5 Citations (Scopus)

Abstract

We synthesized (+)-decursin derivatives substituted with cinnamoyl- and phenyl propionyl groups originating from (+)-CGK062 and screened them using a cell-based assay to detect relative luciferase reporter activity. Of this series, compound 8b, in which a 3-acetoxy cinnamoyl group was introduced, most potently inhibited (97.0%) the Wnt/β-catenin pathway. Specifically, compound 8b dose-dependently inhibited Wnt3a-induced expression of the β-catenin response transcription (CRT) and increased β-catenin degradation in HEK293 reporter cells. Furthermore, compound 8b suppressed expression of the downstream β-catenin target genes cyclin D1 and c-myc and suppressed PC3 cell growth in a concentration-dependent manner.

Original languageEnglish
Pages (from-to)3529-3532
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume26
Issue number15
DOIs
Publication statusPublished - 2016

Keywords

  • Cinnamoyl decursin
  • Phenylpropionyl decursin
  • Prostate cancer
  • Protein degradation
  • Wnt/β-catenin pathway

ASJC Scopus subject areas

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

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