Novel pyrazinone mono-amides as potent and reversible caspase-3 inhibitors

  • Bioorg Med Chem Lett. 2005 Feb 15;15(4):1173-80. doi: 10.1016/j.bmcl.2004.12.006.
Yongxin Han  1 ,  André Giroux ,  John Colucci ,  Christopher I Bayly ,  Daniel J Mckay ,  Sophie Roy ,  Steve Xanthoudakis ,  John Vaillancourt ,  Dita M Rasper ,  John Tam ,  Paul Tawa ,  Donald W Nicholson ,  Robert J Zamboni
Affiliations
  • 1. Department of Medicinal Chemistry, Merck Frosst Centre for Therapeutic Research, Merck Frosst Canada & Co., PO Box 1005, Pointe-Claire-Dorval, Quebec, Canada H9R 4P8. [email protected]
PMID: 15686936 DOI: 10.1016/j.bmcl.2004.12.006
Abstract

The iterative process for the discovery of a series of pyrazinone mono-amides as potent, selective and reversible non-peptide Caspase-3 inhibitors (e.g., M826 and M867) is reported. These compounds display potent anti apoptotic activities in a number of cell based systems in vitro as well as in several animal models in vivo.

Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-155613
    M867
    Caspase-3 Inhibitor
    target: Caspase
    Research Areas: Cancer