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Bioorg Med Chem Lett ; 24(3): 790-3, 2014 Feb 01.
Article in English | MEDLINE | ID: mdl-24433860

ABSTRACT

Inhibition of the phosphoinositide 3-kinase (PI3K)/AKT/mammalian target of rapamycin (mTOR) signaling pathway is one of the most intensively studied approaches to cancer therapy. Rational design led to the identification of novel 7-amino-5-methyl-1,6-naphthyridin-2(1H)-one derivatives as potent PI3K/mTOR dual inhibitors. Design, synthesis and structure activity relationship are reported.


Subject(s)
Drug Design , Naphthyridines/chemistry , Naphthyridines/pharmacology , Phosphoinositide-3 Kinase Inhibitors , Protein Kinase Inhibitors/pharmacology , TOR Serine-Threonine Kinases/antagonists & inhibitors , Animals , Binding Sites , Enzyme Activation/drug effects , Inhibitory Concentration 50 , Mice , Molecular Structure , Naphthyridines/pharmacokinetics , Protein Kinase Inhibitors/chemistry , Protein Kinase Inhibitors/isolation & purification , Signal Transduction/drug effects , Structure-Activity Relationship
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