Identification of a Potent Phosphoinositide 3‐Kinase Pan Inhibitor Displaying a Strategic Carboxylic Acid Group and Development of Its Prodrugs

Activation of the phosphoinositide 3‐kinase (PI3K) pathway is a key signaling event in cancer, inflammation, and other proliferative diseases. PI3K inhibitors are already approved for some specific clinical indications, but their systemic on‐target toxicity limits their larger use. In particular, wh...

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Veröffentlicht in:	ChemMedChem 2017-09, Vol.12 (18), p.1542-1554
Hauptverfasser:	Pirali, Tracey, Ciraolo, Elisa, Aprile, Silvio, Massarotti, Alberto, Berndt, Alex, Griglio, Alessia, Serafini, Marta, Mercalli, Valentina, Landoni, Clarissa, Campa, Carlo Cosimo, Margaria, Jean Piero, Silva, Rangel L., Grosa, Giorgio, Sorba, Giovanni, Williams, Roger, Hirsch, Emilio, Tron, Gian Cesare
Format:	Artikel
Sprache:	eng
Schlagworte:	1-Phosphatidylinositol 3-kinase Animals Binding Sites Cancer Carboxylic acids Carboxylic Acids - chemistry Carboxylic Acids - metabolism Carboxylic Acids - pharmacology Cell Line, Tumor Cell Proliferation - drug effects Chemical compounds Chronic conditions Chronic illnesses click chemistry Drug Design Drugs Enzyme inhibitors Enzyme Inhibitors - chemistry Enzyme Inhibitors - metabolism Enzyme Inhibitors - pharmacology Group dynamics Humans Hydrogen Bonding inflammation Inhibitors Inhibitory Concentration 50 Isoforms Leukocytes Libraries Mice Microsomes - metabolism Molecular Dynamics Simulation nitrogen heterocycles Phosphatidylinositol 3-Kinases - metabolism phosphoinositide 3-kinases Phosphoinositide-3 Kinase Inhibitors Prodrugs Prodrugs - chemistry Prodrugs - metabolism Prodrugs - pharmacology Protein Binding Protein Isoforms - antagonists & inhibitors Protein Isoforms - metabolism Quinolones - chemistry Quinolones - metabolism Quinolones - pharmacology Redundancy Structure-Activity Relationship Toxicity
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