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

Bioorg Med Chem Lett. 2012 Mar 1;22(5):1874-8. doi: 10.1016/j.bmcl.2012.01.074. Epub 2012 Jan 28.

Abstract

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / metabolism
  • Antineoplastic Agents / pharmacology
  • Cell Line, Tumor
  • Humans
  • Imidazoles / chemistry*
  • Imidazoles / metabolism
  • Imidazoles / pharmacology*
  • Mice
  • Microsomes, Liver / metabolism
  • Models, Molecular
  • Neoplasms / drug therapy
  • Neoplasms / enzymology
  • Phosphatidylinositol 3-Kinases / metabolism
  • Phosphoinositide-3 Kinase Inhibitors*
  • 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 / chemistry*
  • Pyrazines / metabolism
  • Pyrazines / pharmacology*
  • Signal Transduction / drug effects

Substances

  • Antineoplastic Agents
  • Imidazoles
  • Phosphoinositide-3 Kinase Inhibitors
  • Protein Kinase Inhibitors
  • Pyrazines
  • imidazo(1,2-a)pyrazine
  • Proto-Oncogene Proteins c-akt