Abstract
Phosphatidylinositol-3-kinase α (PI3Kα) is a therapeutic target of high interest in anticancer drug research. On the basis of a binding model rationalizing the high selectivity and potency of a particular series of 2-aminothiazole compounds in inhibiting PI3Kα, a medicinal chemistry program has led to the discovery of the clinical candidate NVP-BYL719.
Copyright © 2013 Elsevier Ltd. All rights reserved.
MeSH terms
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Animals
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Biological Availability
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Cell Line
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Dogs
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Dose-Response Relationship, Drug
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Drug Discovery*
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Female
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Humans
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Mice
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Models, Molecular
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Molecular Structure
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Phosphatidylinositol 3-Kinases / metabolism
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Phosphoinositide-3 Kinase Inhibitors*
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Phosphorylation / drug effects
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Protein Kinase Inhibitors / chemical synthesis
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Protein Kinase Inhibitors / chemistry
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Protein Kinase Inhibitors / pharmacology*
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Proto-Oncogene Proteins c-akt / antagonists & inhibitors
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Proto-Oncogene Proteins c-akt / metabolism
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Rats
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Rats, Sprague-Dawley
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Structure-Activity Relationship
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Thiazoles / chemical synthesis
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Thiazoles / chemistry
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Thiazoles / pharmacology*
Substances
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Phosphoinositide-3 Kinase Inhibitors
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Protein Kinase Inhibitors
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Thiazoles
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Alpelisib
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Proto-Oncogene Proteins c-akt