Structure-based design and synthesis of pyrrole derivatives as MEK inhibitors

Bioorg Med Chem Lett. 2010 Jul 15;20(14):4156-8. doi: 10.1016/j.bmcl.2010.05.058. Epub 2010 May 20.

Abstract

A novel series of pyrrole inhibitors of MEK kinase has been developed using structure-based drug design. Optimization of the series led to the identification of potent inhibitors with good pharmaceutical properties.

Publication types

  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Animals
  • Crystallography, X-Ray
  • Drug Design
  • MAP Kinase Kinase Kinases / antagonists & inhibitors*
  • Models, Molecular
  • Molecular Structure
  • Protein Kinase Inhibitors / chemical synthesis
  • Protein Kinase Inhibitors / chemistry*
  • Protein Kinase Inhibitors / pharmacology
  • Pyrroles / chemical synthesis
  • Pyrroles / chemistry*
  • Pyrroles / pharmacology
  • Rats

Substances

  • Protein Kinase Inhibitors
  • Pyrroles
  • MAP Kinase Kinase Kinases