Synthesis and evaluation of (+)-decursin derivatives as inhibitors of the Wnt/beta-catenin pathway
- Authors
- Lee, Jee-Hyun; Kim, Min-Ah; Park, Seoyoung; Cho, Soo-Hyun; Yun, Eunju; O, Yu-Seok; Kim, Jiseon; Goo, Ja-Il; Yun, Mi-Young; Choi, Yongseok; Oh, Sangtaek; Song, Gyu-Yong
- Issue Date
- 1-8월-2016
- Publisher
- PERGAMON-ELSEVIER SCIENCE LTD
- Keywords
- Cinnamoyl decursin; Phenylpropionyl decursin; Wnt/beta-catenin pathway; Prostate cancer; Protein degradation
- Citation
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.26, no.15, pp.3529 - 3532
- Indexed
- SCIE
SCOPUS
- Journal Title
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
- Volume
- 26
- Number
- 15
- Start Page
- 3529
- End Page
- 3532
- URI
- https://scholar.korea.ac.kr/handle/2021.sw.korea/87854
- DOI
- 10.1016/j.bmcl.2016.06.029
- ISSN
- 0960-894X
- 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/beta-catenin pathway. Specifically, compound 8b dose-dependently inhibited Wnt3a-induced expression of the beta-catenin response transcription (CRT) and increased beta-catenin degradation in HEK293 reporter cells. Furthermore, compound 8b suppressed expression of the downstream b-catenin target genes cyclin D1 and c-myc and suppressed PC3 cell growth in a concentration-dependent manner. (C) 2016 Published by Elsevier Ltd.
- Files in This Item
- There are no files associated with this item.
- Appears in
Collections - Graduate School > Department of Biotechnology > 1. Journal Articles
Items in ScholarWorks are protected by copyright, with all rights reserved, unless otherwise indicated.