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

Jianming Lu, Zhiqiang Ma, Jen Chieh Hsieh, Chih Wei Fan, Baozhi Chen, Jamie C. Longgood, Noelle S. Williams, James F. Amatruda, Lawrence Lum, Chuo Chen

Research output: Contribution to journalArticle

88 Citations (Scopus)

Abstract

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.

Original languageEnglish (US)
Pages (from-to)3825-3827
Number of pages3
JournalBioorganic and Medicinal Chemistry Letters
Volume19
Issue number14
DOIs
StatePublished - Jul 15 2009

Fingerprint

Structure-Activity Relationship
Molecules
Neoplasms
Therapeutics

Keywords

  • Inhibitor
  • IWR
  • SAR
  • Wnt

ASJC Scopus subject areas

  • Pharmaceutical Science
  • Drug Discovery
  • Organic Chemistry
  • Molecular Medicine
  • Molecular Biology
  • Clinical Biochemistry
  • Biochemistry

Cite this

Structure-activity relationship studies of small-molecule inhibitors of Wnt response. / 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.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 19, No. 14, 15.07.2009, p. 3825-3827.

Research output: Contribution to journalArticle

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. / Structure-activity relationship studies of small-molecule inhibitors of Wnt response. In: Bioorganic and Medicinal Chemistry Letters. 2009 ; Vol. 19, No. 14. pp. 3825-3827.
@article{2e1f94d146c64ee08b92f4478d12dd80,
title = "Structure-activity relationship studies of small-molecule inhibitors of Wnt response",
abstract = "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.",
keywords = "Inhibitor, IWR, SAR, Wnt",
author = "Jianming Lu and Zhiqiang Ma and Hsieh, {Jen Chieh} and Fan, {Chih Wei} and Baozhi Chen and Longgood, {Jamie C.} and Williams, {Noelle S.} and Amatruda, {James F.} and Lawrence Lum and Chuo Chen",
year = "2009",
month = "7",
day = "15",
doi = "10.1016/j.bmcl.2009.04.040",
language = "English (US)",
volume = "19",
pages = "3825--3827",
journal = "Bioorganic and Medicinal Chemistry Letters",
issn = "0960-894X",
publisher = "Elsevier Limited",
number = "14",

}

TY - JOUR

T1 - Structure-activity relationship studies of small-molecule inhibitors of Wnt response

AU - Lu, Jianming

AU - Ma, Zhiqiang

AU - Hsieh, Jen Chieh

AU - Fan, Chih Wei

AU - Chen, Baozhi

AU - Longgood, Jamie C.

AU - Williams, Noelle S.

AU - Amatruda, James F.

AU - Lum, Lawrence

AU - Chen, Chuo

PY - 2009/7/15

Y1 - 2009/7/15

N2 - 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.

AB - 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.

KW - Inhibitor

KW - IWR

KW - SAR

KW - Wnt

UR - http://www.scopus.com/inward/record.url?scp=67649651945&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=67649651945&partnerID=8YFLogxK

U2 - 10.1016/j.bmcl.2009.04.040

DO - 10.1016/j.bmcl.2009.04.040

M3 - Article

C2 - 19410457

AN - SCOPUS:67649651945

VL - 19

SP - 3825

EP - 3827

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

SN - 0960-894X

IS - 14

ER -