Acyl dipeptides as reversible caspase inhibitors. Part 2: further optimization

Bioorg Med Chem Lett. 2002 Oct 21;12(20):2973-5. doi: 10.1016/s0960-894x(02)00630-3.

Abstract

A new structural class of broad spectrum caspase inhibitors was optimized for its activity against caspases 1, 3, 6, 7, and 8. The most potent compound had low nanomolar broad spectrum activity, in particular, single digit nanomolar inhibitory activity against caspase 8.

MeSH terms

  • Acylation
  • Caspase Inhibitors*
  • Dipeptides / chemical synthesis*
  • Dipeptides / pharmacology*
  • Enzyme Inhibitors / chemical synthesis*
  • Enzyme Inhibitors / pharmacology*
  • Indicators and Reagents
  • Isoenzymes / antagonists & inhibitors
  • Oligopeptides / chemical synthesis
  • Oligopeptides / pharmacology
  • Structure-Activity Relationship

Substances

  • Caspase Inhibitors
  • Dipeptides
  • Enzyme Inhibitors
  • Indicators and Reagents
  • Isoenzymes
  • Oligopeptides