Abstract
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.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, Non-U.S. Gov't
MeSH terms
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Antineoplastic Agents / chemistry*
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Antineoplastic Agents / pharmacology*
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Cell Line, Tumor
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Cell Proliferation / drug effects*
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Extracellular Signal-Regulated MAP Kinases / antagonists & inhibitors*
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Extracellular Signal-Regulated MAP Kinases / metabolism
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HeLa Cells
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Humans
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MAP Kinase Signaling System / drug effects
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Melanoma / drug therapy*
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Melanoma / enzymology
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Structure-Activity Relationship
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Thiazolidinediones / chemistry*
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Thiazolidinediones / pharmacology*
Substances
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3-(2-aminoethyl)-5-(4-ethoxybenzylidene)thiazolidine-2,4-dione
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Antineoplastic Agents
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Thiazolidinediones
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Extracellular Signal-Regulated MAP Kinases