Literature DB >> 15686936

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

Yongxin Han1, 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.   

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.

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Year:  2005        PMID: 15686936     DOI: 10.1016/j.bmcl.2004.12.006

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  6 in total

Review 1.  Small Molecule Active Site Directed Tools for Studying Human Caspases.

Authors:  Marcin Poreba; Aleksandra Szalek; Paulina Kasperkiewicz; Wioletta Rut; Guy S Salvesen; Marcin Drag
Journal:  Chem Rev       Date:  2015-11-09       Impact factor: 60.622

2.  Neuronal cell death in neonatal hypoxia-ischemia.

Authors:  Frances J Northington; Raul Chavez-Valdez; Lee J Martin
Journal:  Ann Neurol       Date:  2011-05       Impact factor: 10.422

3.  Targeting TNF-alpha receptors for neurotherapeutics.

Authors:  Wayne Chadwick; Tim Magnus; Bronwen Martin; Aleksander Keselman; Mark P Mattson; Stuart Maudsley
Journal:  Trends Neurosci       Date:  2008-09-04       Impact factor: 13.837

4.  Radiosensitization of solid tumors by Z-VAD, a pan-caspase inhibitor.

Authors:  Luigi Moretti; Kwang Woon Kim; Dae Kwang Jung; Christopher D Willey; Bo Lu
Journal:  Mol Cancer Ther       Date:  2009-05-05       Impact factor: 6.261

5.  M867, a novel selective inhibitor of caspase-3 enhances cell death and extends tumor growth delay in irradiated lung cancer models.

Authors:  Kwang Woon Kim; Luigi Moretti; Bo Lu
Journal:  PLoS One       Date:  2008-05-28       Impact factor: 3.240

6.  De Novo Molecular Design of Caspase-6 Inhibitors by a GRU-Based Recurrent Neural Network Combined with a Transfer Learning Approach.

Authors:  Shuheng Huang; Hu Mei; Laichun Lu; Minyao Qiu; Xiaoqi Liang; Lei Xu; Zuyin Kuang; Yu Heng; Xianchao Pan
Journal:  Pharmaceuticals (Basel)       Date:  2021-11-30
  6 in total

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