Abstract
A series of [1,2,4]triazolo[3,4-f][1,6]naphthyridine allosteric dual inhibitors of Akt1 and 2 have been developed. These compounds have been shown to have potent dual Akt1 and 2 cell potency. The representative compound 13 provided potent inhibitory activity against Akt1 and 2 in vivo in a mouse model.
MeSH terms
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Allosteric Site
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Animals
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Chemistry, Pharmaceutical / methods*
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Dose-Response Relationship, Drug
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Drug Design
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ERG1 Potassium Channel
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Ether-A-Go-Go Potassium Channels / metabolism
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Inhibitory Concentration 50
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Lung / drug effects
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Mice
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Models, Chemical
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Naphthyridines / chemistry*
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Proto-Oncogene Proteins c-akt / antagonists & inhibitors*
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Proto-Oncogene Proteins c-akt / chemistry
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Structure-Activity Relationship
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Triazoles / chemistry*
Substances
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ERG1 Potassium Channel
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Ether-A-Go-Go Potassium Channels
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Naphthyridines
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Triazoles
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Proto-Oncogene Proteins c-akt