Achieving multi-isoform PI3K inhibition in a series of substituted 3,4-dihydro-2H-benzo[1,4]oxazines

The SAR and pharmacokinetic profiles of a series of multi-isoform PI3K inhibitors based on a 3,4-dihydro-2H-benzo[1,4]oxazine scaffold are disclosed. The SAR and pharmacokinetic profiles of a series of multi-isoform PI3K inhibitors based on a 3,4-dihydro-2H-benzo[1,4]oxazine scaffold are disclosed.

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Bibliographic Details
Published in:	Bioorganic & medicinal chemistry Vol. 18; no. 16; pp. 4700 - 4704
Main Authors:	Perry, Benjamin, Alexander, Rikki, Bennett, Gavin, Buckley, George, Ceska, Tom, Crabbe, Tom, Dale, Verity, Gowers, Lewis, Horsley, Helen, James, Lynwen, Jenkins, Kerry, Crépy, Karen, Kulisa, Claire, Lightfoot, Helen, Lock, Chris, Mack, Stephen, Morgan, Trevor, Nicolas, Anne-Lise, Pitt, Will, Sabin, Verity, Wright, Sara
Format:	Journal Article
Language:	English
Published:	Oxford Elsevier Ltd 15-08-2008 Elsevier
Subjects:	Area Under Curve Benzoxazines - chemistry Benzoxazines - pharmacology Biological and medical sciences Bones, joints and connective tissue. Antiinflammatory agents Chemistry, Pharmaceutical - methods Crystallography, X-Ray - methods Drug Design Humans Inflammation Inhibitory Concentration 50 Isoform Kinase Medical sciences Models, Chemical Molecular Structure Oxazines - chemical synthesis Oxazines - pharmacology Pharmacology. Drug treatments Phosphatidylinositol 3-Kinases - metabolism PI3K Protein Isoforms Small molecule Structure-Activity Relationship Isoform Inflammation Small molecule PI3K Kinase Intravenous administration Rat Nitrogen heterocycle Isozyme Lactam Pyridine derivatives Signal transduction Structure activity relation Bicyclic compound Pyrazole derivatives Pyridazine derivatives Aromatic compound Chemical synthesis Oxygen nitrogen heterocycle Sulfur nitrogen heterocycle Enzyme Transferases Rodentia Antiinflammatory agent Oral administration Enzyme inhibitor Ketone In vitro 1-Phosphatidylinositol 3-kinase In vivo Vertebrata Mammalia Animal Pharmacokinetics P13K
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Summary:	The SAR and pharmacokinetic profiles of a series of multi-isoform PI3K inhibitors based on a 3,4-dihydro-2H-benzo[1,4]oxazine scaffold are disclosed. The SAR and pharmacokinetic profiles of a series of multi-isoform PI3K inhibitors based on a 3,4-dihydro-2H-benzo[1,4]oxazine scaffold are disclosed.
Bibliography:	ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23
ISSN:	0960-894X 0968-0896 1464-3405 1464-3391
DOI:	10.1016/j.bmcl.2008.06.104