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

Bioorg Med Chem Lett. 2008 Aug 15;18(16):4700-4. doi: 10.1016/j.bmcl.2008.06.104. Epub 2008 Jul 5.

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.

MeSH terms

  • Area Under Curve
  • Benzoxazines / chemistry*
  • Benzoxazines / pharmacology
  • Chemistry, Pharmaceutical / methods*
  • Crystallography, X-Ray / methods
  • Drug Design
  • Humans
  • Inflammation
  • Inhibitory Concentration 50
  • Models, Chemical
  • Molecular Structure
  • Oxazines / chemical synthesis*
  • Oxazines / pharmacology*
  • Phosphatidylinositol 3-Kinases / metabolism*
  • Protein Isoforms
  • Structure-Activity Relationship

Substances

  • Benzoxazines
  • Oxazines
  • Protein Isoforms
  • Phosphatidylinositol 3-Kinases