Entry into a new class of protein kinase inhibitors by pseudo ring design

Bioorg Med Chem Lett. 2008 Feb 1;18(3):897-900. doi: 10.1016/j.bmcl.2007.12.041. Epub 2008 Jan 14.

Abstract

A pyrimidin-4-yl-urea motif forming a pseudo ring by intramolecular hydrogen bonding has been designed to mimic the pyrido[2,3-d]pyrimidin-7-one core structure of a well-established class of protein kinase inhibitors. Potent inhibition of a number of protein kinases was obtained with the first prototype compound synthesized to probe the design concept.

MeSH terms

  • Amino Acids / chemistry
  • Amino Acids / pharmacology
  • Drug Design*
  • Models, Molecular*
  • Molecular Conformation
  • Molecular Mimicry
  • Molecular Structure
  • Protein Kinase Inhibitors / chemical synthesis*
  • Protein Kinase Inhibitors / chemistry
  • Protein Kinase Inhibitors / pharmacology*
  • Pyridones / chemistry*
  • Pyridones / pharmacology*
  • Pyrimidines / chemical synthesis*
  • Pyrimidines / chemistry
  • Pyrimidines / pharmacology*
  • Structure-Activity Relationship
  • Urea / analogs & derivatives*
  • Urea / chemical synthesis*
  • Urea / chemistry
  • Urea / pharmacology*

Substances

  • Amino Acids
  • PD 166285
  • Protein Kinase Inhibitors
  • Pyridones
  • Pyrimidines
  • Urea