Aminofurazans as potent inhibitors of AKT kinase

Bioorg Med Chem Lett. 2009 Mar 1;19(5):1508-11. doi: 10.1016/j.bmcl.2009.01.002. Epub 2009 Jan 9.

Abstract

AKT inhibitors containing an imidazopyridine aminofurazan scaffold have been optimized. We have previously disclosed identification of the AKT inhibitor GSK690693, which has been evaluated in clinical trials in cancer patients. Herein we describe recent efforts focusing on investigating a distinct region of this scaffold that have afforded compounds (30 and 32) with comparable activity profiles to that of GSK690693.

Publication types

  • Comparative Study

MeSH terms

  • Animals
  • Cell Line
  • Cell Line, Tumor
  • Crystallography, X-Ray
  • Humans
  • Oxadiazoles / chemical synthesis*
  • Oxadiazoles / chemistry
  • Oxadiazoles / pharmacology
  • Oxadiazoles / therapeutic use
  • Protein Kinase Inhibitors / chemical synthesis*
  • Protein Kinase Inhibitors / pharmacology
  • Protein Structure, Secondary / physiology
  • Proto-Oncogene Proteins c-akt / antagonists & inhibitors*
  • Proto-Oncogene Proteins c-akt / metabolism
  • Structure-Activity Relationship

Substances

  • GSK690693
  • Oxadiazoles
  • Protein Kinase Inhibitors
  • Proto-Oncogene Proteins c-akt