Discovery of a new class of p38 kinase inhibitors

Bioorg Med Chem Lett. 2000 Sep 18;10(18):2047-50. doi: 10.1016/s0960-894x(00)00270-5.

Abstract

The MAP kinase p38 has been implicated in cytokine signaling, and its inhibitors are potentially useful for the treatment of arthritis and osteoporosis. Novel small-molecule inhibitors of p38 kinase were derived from a combinatorial chemistry effort and exhibit activity in the nanomolar range. Very steep structure-activity relationships are observed within this class.

MeSH terms

  • Antirheumatic Agents / chemical synthesis
  • Antirheumatic Agents / chemistry
  • Combinatorial Chemistry Techniques
  • Enzyme Inhibitors / chemical synthesis*
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / pharmacology
  • Heterocyclic Compounds / chemistry
  • Humans
  • Hydrocarbons, Chlorinated / chemistry
  • Inhibitory Concentration 50
  • Mitogen-Activated Protein Kinases / antagonists & inhibitors*
  • Osteoporosis / drug therapy
  • Phenylurea Compounds / chemical synthesis
  • Phenylurea Compounds / pharmacology
  • Structure-Activity Relationship
  • p38 Mitogen-Activated Protein Kinases

Substances

  • Antirheumatic Agents
  • Enzyme Inhibitors
  • Heterocyclic Compounds
  • Hydrocarbons, Chlorinated
  • Phenylurea Compounds
  • Mitogen-Activated Protein Kinases
  • p38 Mitogen-Activated Protein Kinases