Identification of novel pyrrolopyrazoles as protein kinase C β II inhibitors

Bioorg Med Chem Lett. 2011 Jan 1;21(1):584-7. doi: 10.1016/j.bmcl.2010.10.032. Epub 2010 Oct 13.

Abstract

A novel series of pyrrolopyrazole-based protein kinase C β II inhibitors has been identified from high-throughput screening. Herein, we report our initial structure-activity relationship studies with a focus on optimizing compound ligand efficiency and physicochemical properties, which has led to potent inhibitors with good cell permeability.

MeSH terms

  • High-Throughput Screening Assays
  • Protein Kinase C / antagonists & inhibitors*
  • Protein Kinase C / metabolism
  • Protein Kinase C beta
  • Protein Kinase Inhibitors / chemical synthesis
  • Protein Kinase Inhibitors / chemistry*
  • Protein Kinase Inhibitors / pharmacology
  • Pyrazoles / chemical synthesis
  • Pyrazoles / chemistry*
  • Pyrazoles / pharmacology
  • Structure-Activity Relationship

Substances

  • Protein Kinase Inhibitors
  • Pyrazoles
  • Protein Kinase C
  • Protein Kinase C beta