کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1368507 981701 2016 4 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Synthesis and evaluation of (+)-decursin derivatives as inhibitors of the Wnt/β-catenin pathway
ترجمه فارسی عنوان
سنتز و ارزيابي مشتقات (+) - ديكورسين به عنوان بازدارنده هاي مسیر Wnt / β-catenin
کلمات کلیدی
Cinnamoyl deursin؛ decursin Phenylpropionyl؛ مسیر Wnt / β-catenin؛ سرطان پروستات؛ تخریب پروتئین
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
چکیده انگلیسی

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.

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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 26, Issue 15, 1 August 2016, Pages 3529–3532
نویسندگان
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