Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor

Phosphoinositide-3-kinase (PI3K) is an important target for cancer therapeutics due to the deregulation of this signaling pathway in a wide variety of human cancers. Herein, we describe the optimization of imidazo [1,2-a] pyrazines, which allow us to identify compound 14 (ETP-46321), with potent bio...

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Bibliographic Details
Published in:	Bioorganic & medicinal chemistry letters Vol. 22; no. 10; pp. 3460 - 3466
Main Authors:	Martínez González, Sonia, Hernández, Ana Isabel, Varela, Carmen, Rodríguez-Arístegui, Sonsoles, Lorenzo, Milagros, Rodríguez, Antonio, Rivero, Virginia, Martín, José Ignacio, Saluste, Carl Gustav, Ramos-Lima, Francisco, Cendón, Elena, Cebrián, David, Aguirre, Enara, Gomez-Casero, Elena, Albarrán, Maribel, Alfonso, Patricia, García-Serelde, Beatriz, Oyarzabal, Julen, Rabal, Obdulia, Mulero, Francisca, Gonzalez-Granda, Teresa, Link, Wolfgang, Fominaya, Jesús, Barbacid, Mariano, Bischoff, James R., Pizcueta, Pilar, Pastor, Joaquín
Format:	Journal Article
Language:	English
Published:	Amsterdam Elsevier Ltd 15-05-2012 Elsevier
Subjects:	Administration, Oral Biological and medical sciences Biological Availability Cancer treatment gene expression regulation growth retardation Humans Imidazoles - administration & dosage Imidazoles - pharmacokinetics Imidazoles - pharmacology Isoenzymes - antagonists & inhibitors Medical sciences mice mutation neoplasms pharmacokinetics Pharmacology. Drug treatments phosphatidylinositol 3-kinase Phosphatidylinositol 3-Kinases - antagonists & inhibitors phosphorylation PI3K inhibitors Positron-Emission Tomography Protein Kinase Inhibitors - administration & dosage Protein Kinase Inhibitors - pharmacokinetics Protein Kinase Inhibitors - pharmacology pyrazines Pyrazines - administration & dosage Pyrazines - pharmacokinetics Pyrazines - pharmacology signal transduction therapeutics Tomography, X-Ray Computed PI3K inhibitors Cancer treatment Antineoplastic agent Signal transduction Enzyme Transferases Oral administration Inhibitor Bioavailability Pharmacokinetics 1-Phosphatidylinositol 3-kinase
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