2. Academic Validation
  3. Synthesis and evaluation of (+)-decursin derivatives as inhibitors of the Wnt/β-catenin pathway

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

  • Bioorg Med Chem Lett. 2016 Aug 1;26(15):3529-32. doi: 10.1016/j.bmcl.2016.06.029.
Jee-Hyun Lee 1,  Min-Ah Kim 1,  Seoyoung Park 2,  Soo-Hyun Cho 1,  Eunju Yun 1,  Yu-Seok O 1,  Jiseon Kim 1,  Ja-Il Goo 3,  Mi-Young Yun 4,  Yongseok Choi 3,  Sangtaek Oh 5,  Gyu-Yong Song 6
Affiliations

Affiliations

  • 1 College of Pharmacy, Chungnam National University, Daejeon 305-764, Republic of Korea.
  • 2 Department of Bio and Fermentation Convergence Technology, Kookmin University, Seoul 136-702, Republic of Korea.
  • 3 College of Life Sciences and Biotechnology, Korea University, Seoul 136-701, Republic of Korea.
  • 4 Department of Beauty Science, Kwangju Women's University, Kwangju 506-713, Republic of Korea.
  • 5 Department of Bio and Fermentation Convergence Technology, Kookmin University, Seoul 136-702, Republic of Korea. Electronic address: ohsa@kookmin.ac.kr.
  • 6 College of Pharmacy, Chungnam National University, Daejeon 305-764, Republic of Korea. Electronic address: gysong@cnu.ac.kr.
PMID: 27329797 DOI: 10.1016/j.bmcl.2016.06.029
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.

Keywords

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

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