"Click" synthesis of small-molecule inhibitors targeting caspases

Org Biomol Chem. 2008 Mar 7;6(5):844-7. doi: 10.1039/b718304f. Epub 2008 Feb 4.

Abstract

A panel of 198 P4-diversified aldehyde (reversible) and vinyl sulfone (irreversible) inhibitors is successfully synthesized via an efficient "click chemistry" platform and directly screened against caspase-3 and -7 for inhibition.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aldehydes / chemical synthesis*
  • Aldehydes / chemistry
  • Aldehydes / pharmacology
  • Caspase Inhibitors*
  • Drug Design*
  • Enzyme Inhibitors / chemical synthesis*
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / pharmacology
  • Inhibitory Concentration 50
  • Molecular Conformation
  • Molecular Weight
  • Small Molecule Libraries / chemical synthesis*
  • Stereoisomerism
  • Structure-Activity Relationship
  • Sulfones / chemical synthesis*
  • Sulfones / chemistry
  • Sulfones / pharmacology

Substances

  • Aldehydes
  • Caspase Inhibitors
  • Enzyme Inhibitors
  • Small Molecule Libraries
  • Sulfones
  • divinyl sulfone