4-(1,3-Thiazol-2-yl)morpholine derivatives as inhibitors of phosphoinositide 3-kinase

Bioorg Med Chem Lett. 2008 Aug 1;18(15):4316-20. doi: 10.1016/j.bmcl.2008.06.076. Epub 2008 Jun 28.

Abstract

4-(1,3-Thiazol-2-yl)morpholine derivatives have been identified as potent and selective inhibitors of phosphoinositide 3-kinase. The SAR data of selected examples are presented and the in vivo profiling of compound 18 is shown to demonstrate the utility of this class of compounds in xenograft models of tumor growth.

MeSH terms

  • 1-Phosphatidylinositol 4-Kinase / antagonists & inhibitors*
  • Animals
  • Combinatorial Chemistry Techniques
  • Drug Screening Assays, Antitumor
  • Humans
  • Isoenzymes
  • Mice
  • Molecular Structure
  • Morpholines / chemical synthesis
  • Morpholines / chemistry
  • Morpholines / pharmacology*
  • Structure-Activity Relationship
  • Thiazoles / chemical synthesis
  • Thiazoles / chemistry
  • Thiazoles / pharmacology*
  • Xenograft Model Antitumor Assays

Substances

  • Isoenzymes
  • Morpholines
  • Thiazoles
  • 1-Phosphatidylinositol 4-Kinase