Imidazo[1,2-a]pyrazines as novel PI3K inhibitors

Phosphoinositide-3-kinase (PI3K) is an important target for cancer therapeutics due to the deregulation of its signaling pathway in a wide variety of human cancers. We describe herein a novel series of imidazo[1,2-a]pyrazines as PI3K inhibitors.

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2012-03, Vol.22 (5), p.1874-1878
Hauptverfasser:	Martínez González, Sonia, Hernández, Ana Isabel, Varela, Carmen, Rodríguez-Arístegui, Sonsoles, Alvarez, Rosa María, García, Ana Belén, Lorenzo, Milagros, Rivero, Virginia, Oyarzabal, Julen, Rabal, Obdulia, Bischoff, James R., Albarrán, Maribel, Cebriá, Antonio, Alfonso, Patricia, Link, Wolfgang, Fominaya, Jesús, Pastor, Joaquín
Format:	Artikel
Sprache:	eng
Schlagworte:	8-Morpholinyl Imidazo[1,2-a]pyrazines Animals Antineoplastic Agents - chemistry Antineoplastic Agents - metabolism Antineoplastic Agents - pharmacology Biological and medical sciences Cancer treatment Cell Line, Tumor chemistry Humans Imidazoles - chemistry Imidazoles - metabolism Imidazoles - pharmacology Medical sciences Mice Microsomes, Liver - metabolism Models, Molecular neoplasms Neoplasms - drug therapy Neoplasms - enzymology p110 α,β,δ,γ P13K inhibitors Pharmacology. Drug treatments phosphatidylinositol 3-kinase Phosphatidylinositol 3-Kinases - antagonists & inhibitors Phosphatidylinositol 3-Kinases - metabolism Protein Kinase Inhibitors - chemistry Protein Kinase Inhibitors - metabolism Protein Kinase Inhibitors - pharmacology Proto-Oncogene Proteins c-akt - antagonists & inhibitors Proto-Oncogene Proteins c-akt - metabolism pyrazines Pyrazines - chemistry Pyrazines - metabolism Pyrazines - pharmacology signal transduction Signal Transduction - drug effects therapeutics
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Beschreibung
Zusammenfassung:	Phosphoinositide-3-kinase (PI3K) is an important target for cancer therapeutics due to the deregulation of its signaling pathway in a wide variety of human cancers. We describe herein a novel series of imidazo[1,2-a]pyrazines as PI3K inhibitors.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2012.01.074