Structure–activity relationship studies of small-molecule inhibitors of Wnt response

SAR studies of IWR-1 are described. Suppression of oncogenic Wnt-mediated signaling holds promise as an anti-cancer therapeutic strategy. We previously reported a novel class of small molecules (IWR-1/2, inhibitors of Wnt response) that antagonize Wnt signaling by stabilizing the Axin destruction co...

Ausführliche Beschreibung

Gespeichert in:

Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2009-07, Vol.19 (14), p.3825-3827
Hauptverfasser:	Lu, Jianming, Ma, Zhiqiang, Hsieh, Jen-Chieh, Fan, Chih-Wei, Chen, Baozhi, Longgood, Jamie C., Williams, Noelle S., Amatruda, James F., Lum, Lawrence, Chen, Chuo
Format:	Artikel
Sprache:	eng
Schlagworte:	Aminoquinolines - chemistry Animals Antineoplastic agents Axin Protein Biological and medical sciences General aspects Imides - chemistry Inhibitor IWR Medical sciences Pharmacology. Drug treatments Repressor Proteins - metabolism SAR Signal Transduction Structure-Activity Relationship Tail Wnt Wnt Proteins - antagonists & inhibitors Wnt Proteins - metabolism Zebrafish - metabolism
Online-Zugang:	Volltext
Tags:	Tag hinzufügen Keine Tags, Fügen Sie den ersten Tag hinzu!

Beschreibung
Zusammenfassung:	SAR studies of IWR-1 are described. Suppression of oncogenic Wnt-mediated signaling holds promise as an anti-cancer therapeutic strategy. We previously reported a novel class of small molecules (IWR-1/2, inhibitors of Wnt response) that antagonize Wnt signaling by stabilizing the Axin destruction complex. Herein, we present the results of structure-activity relationship studies of these compounds.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2009.04.040