Literature DB >> 18644721

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

Benjamin Perry1, Rikki Alexander, Gavin Bennett, George Buckley, Tom Ceska, Tom Crabbe, Verity Dale, Lewis Gowers, Helen Horsley, Lynwen James, Kerry Jenkins, Karen Crépy, Claire Kulisa, Helen Lightfoot, Chris Lock, Stephen Mack, Trevor Morgan, Anne-Lise Nicolas, Will Pitt, Verity Sabin, Sara Wright.   

Abstract

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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Year:  2008        PMID： 18644721     DOI： 10.1016/j.bmcl.2008.06.104

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  2 in total

Review 1.  Somatic mutations in PI3Kalpha: structural basis for enzyme activation and drug design.

Authors:  Sandra B Gabelli; Diana Mandelker; Oleg Schmidt-Kittler; Bert Vogelstein; L Mario Amzel
Journal:  Biochim Biophys Acta       Date:  2009-12-02

Review 2.  Progress in the preclinical discovery and clinical development of class I and dual class I/IV phosphoinositide 3-kinase (PI3K) inhibitors.

Authors:  S J Shuttleworth; F A Silva; A R L Cecil; C D Tomassi; T J Hill; F I Raynaud; P A Clarke; P Workman
Journal:  Curr Med Chem       Date:  2011       Impact factor: 4.530
  2 in total

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