Document Detail


Structural modifications of (Z)-3-(2-aminoethyl)-5-(4-ethoxybenzylidene)thiazolidine-2,4-dione that improve selectivity for inhibiting the proliferation of melanoma cells containing active ERK signaling.
MedLine Citation:
PMID:  23624850     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
We herein report on the pharmacophore determination of the ERK docking domain inhibitor (Z)-3-(2-aminoethyl)-5-(4-ethoxybenzylidene)thiazolidine-2,4-dione, which has led to the discovery of compounds with greater selectivities for inhibiting the proliferation of melanoma cells containing active ERK signaling.
Authors:
Kwan-Young Jung; Ramin Samadani; Jay Chauhan; Kerrick Nevels; Jeremy L Yap; Jun Zhang; Shilpa Worlikar; Maryanna E Lanning; Lijia Chen; Mary Ensey; Sagar Shukla; Rosene Salmo; Geoffrey Heinzl; Caryn Gordon; Troy Dukes; Alexander D MacKerell; Paul Shapiro; Steven Fletcher
Publication Detail:
Type:  Journal Article; Research Support, N.I.H., Extramural; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Organic & biomolecular chemistry     Volume:  11     ISSN:  1477-0539     ISO Abbreviation:  Org. Biomol. Chem.     Publication Date:  2013 Jun 
Date Detail:
Created Date:  2013-05-14     Completed Date:  2013-11-25     Revised Date:  2013-11-27    
Medline Journal Info:
Nlm Unique ID:  101154995     Medline TA:  Org Biomol Chem     Country:  England    
Other Details:
Languages:  eng     Pagination:  3706-32     Citation Subset:  IM    
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MeSH Terms
Descriptor/Qualifier:
Antineoplastic Agents / chemistry*,  pharmacology*
Cell Line, Tumor
Cell Proliferation / drug effects*
Extracellular Signal-Regulated MAP Kinases / antagonists & inhibitors*,  metabolism
HeLa Cells
Humans
MAP Kinase Signaling System / drug effects
Melanoma / drug therapy*,  enzymology
Structure-Activity Relationship
Thiazolidinediones / chemistry*,  pharmacology*
Grant Support
ID/Acronym/Agency:
CA120215/CA/NCI NIH HHS; F31 GM100693/GM/NIGMS NIH HHS; GM100693/GM/NIGMS NIH HHS; R01 CA120215/CA/NCI NIH HHS
Chemical
Reg. No./Substance:
0/3-(2-aminoethyl)-5-(4-ethoxybenzylidene)thiazolidine-2,4-dione; 0/Antineoplastic Agents; 0/Thiazolidinediones; EC 2.7.11.24/Extracellular Signal-Regulated MAP Kinases

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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