학술논문
Design, Synthesis,and Biological Evaluation of a Series of Anthracene-9,10-dione Dioximeβ-Catenin Pathway Inhibitors.
Document Type
Article
Author
Source
Subject
*DRUG design
*DRUG synthesis
*ANTHRACENE
*CATENINS
*ENZYME inhibitors
*CANCER cell differentiation
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Language
ISSN
0022-2623
Abstract
TheWnt/β-catenin signaling pathway plays a vital role in cell growth,the regulation, cell development, and the differentiation of normalstem cells. Constitutive activation of the Wnt/β-catenin signalingpathway is found in many human cancers, and thus, it is an attractivetarget for anticancer therapy. Specific inhibitors of this pathwayhave been keenly researched and developed. Cell based screening ofcompounds library, hit-to-lead optimization, computational and structure-baseddesign strategies resulted in the design and synthesis of a seriesof anthracene-9,10-dione dioxime series of compounds demonstratedpotent inhibition of β-catenin in vitro (IC50<10 nM, 14) and the growth of several cancer cell lines.This article discusses the potential of inhibiting the Wnt/β-cateninsignaling pathway as a therapeutic approach for cancer along withan overview of the development of specific inhibitors. [ABSTRACT FROM AUTHOR]