Synthesis and evaluation of (+)-decursin derivatives as inhibitors of the Wnt/ß-catenin pathway.
Bioorg Med Chem Lett
; 26(15): 3529-32, 2016 08 01.
Article
em En
| MEDLINE
| ID: mdl-27329797
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/ß-catenin pathway. Specifically, compound 8b dose-dependently inhibited Wnt3a-induced expression of the ß-catenin response transcription (CRT) and increased ß-catenin degradation in HEK293 reporter cells. Furthermore, compound 8b suppressed expression of the downstream ß-catenin target genes cyclin D1 and c-myc and suppressed PC3 cell growth in a concentration-dependent manner.
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Texto completo:
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Benzopiranos
/
Butiratos
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Proteínas Wnt
/
Beta Catenina
Limite:
Humans
Idioma:
En
Ano de publicação:
2016
Tipo de documento:
Article