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ID: ALA3826880
Journal: Bioorg Med Chem Lett
Title: Synthesis and evaluation of (+)-decursin derivatives as inhibitors of the Wnt/β-catenin pathway.
Authors: Lee JH, Kim MA, Park S, Cho SH, Yun E, O YS, Kim J, Goo JI, Yun MY, Choi Y, Oh S, Song GY.
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.
CiteXplore: 27329797