Allosteric inhibitors of Akt1 and Akt2: Discovery of [1,2,4]triazolo[3,4-f][1,6]naphthyridines with potent and balanced activity

Autor:	Stanley F. Barnett, Nicholas D. P. Cosford, Deborah Defeo-Jones, Michael A. Rossi, Jun Liang, Hans E. Huber, Ronald G. Robinson, Raymond E. Jones, Hu Essa H, Yiwei Li, Sachin Mittal, Karen R. Leander, Tony Siu, Peppi Prasit
Rok vydání:	2009
Předmět:	ERG1 Potassium Channel Stereochemistry Chemistry Pharmaceutical Clinical Biochemistry Allosteric regulation Pharmaceutical Science Biochemistry Chemical synthesis Inhibitory Concentration 50 Mice Structure-Activity Relationship In vivo Drug Discovery Animals Naphthyridines Lung Molecular Biology chemistry.chemical_classification Dose-Response Relationship Drug biology Kinase Organic Chemistry Triazoles Ether-A-Go-Go Potassium Channels In vitro Enzyme Models Chemical chemistry Enzyme inhibitor Drug Design embryonic structures biology.protein Molecular Medicine Signal transduction Proto-Oncogene Proteins c-akt Allosteric Site
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 19:834-836
ISSN:	0960-894X
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d5ba20e71cf707c07711af7cafaca26d https://doi.org/10.1016/j.bmcl.2008.12.017 Zobrazit plný text záznamu Full Text from ScienceDirect