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

作者信息

Han Yongxin, Giroux André, Colucci John, Bayly Christopher I, Mckay Daniel J, Roy Sophie, Xanthoudakis Steve, Vaillancourt John, Rasper Dita M, Tam John, Tawa Paul, Nicholson Donald W, Zamboni Robert J

机构信息

Department of Medicinal Chemistry, Merck Frosst Centre for Therapeutic Research, Merck Frosst Canada & Co., PO Box 1005, Pointe-Claire-Dorval, Quebec, Canada H9R 4P8.

出版信息

Bioorg Med Chem Lett. 2005 Feb 15;15(4):1173-80. doi: 10.1016/j.bmcl.2004.12.006.

DOI:10.1016/j.bmcl.2004.12.006

PMID:15686936

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.

摘要

相似文献

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.

1,3-Dioxo-4-methyl-2,3-dihydro-1H-pyrrolo[3,4-c]quinolines as potent caspase-3 inhibitors.

Bioorg Med Chem Lett. 2005 Apr 1;15(7):1841-5. doi: 10.1016/j.bmcl.2005.02.027.

A novel method for evaluation and screening of caspase inhibitory peptides by the amino acid positional fitness score.

BMC Pharmacol. 2004 May 22;4:7. doi: 10.1186/1471-2210-4-7.

Synthesis and evaluation of novel 1-(2-acylhydrazinocarbonyl)-cycloalkyl carboxamides as interleukin-1beta converting enzyme (ICE) inhibitors.

Bioorg Med Chem Lett. 2006 Aug 15;16(16):4233-6. doi: 10.1016/j.bmcl.2006.05.076. Epub 2006 Jun 16.

IRAK-4 inhibitors. Part 1: a series of amides.

Bioorg Med Chem Lett. 2008 Jun 1;18(11):3211-4. doi: 10.1016/j.bmcl.2008.04.058. Epub 2008 Apr 26.

Synthesis and structure-activity relationship of 4-substituted 2-(2-acetyloxyethyl)-8-(morpholine-4-sulfonyl)pyrrolo[3,4-c]quinoline-1,3-diones as potent caspase-3 inhibitors.

J Med Chem. 2005 Jun 2;48(11):3680-3. doi: 10.1021/jm048987t.

Dipyridyl amides: potent metabotropic glutamate subtype 5 (mGlu5) receptor antagonists.

Bioorg Med Chem Lett. 2005 Feb 15;15(4):1197-200. doi: 10.1016/j.bmcl.2004.11.078.

Discovery of novel 2-(aminoheteroaryl)-thiazole-5-carboxamides as potent and orally active Src-family kinase p56(Lck) inhibitors.

Bioorg Med Chem Lett. 2004 Dec 20;14(24):6061-6. doi: 10.1016/j.bmcl.2004.09.093.

Discovery of beta-homophenylalanine based pyrrolidin-2-ylmethyl amides and sulfonamides as highly potent and selective inhibitors of dipeptidyl peptidase IV.

Bioorg Med Chem Lett. 2009 Aug 1;19(15):4201-3. doi: 10.1016/j.bmcl.2009.05.109. Epub 2009 May 30.

Non-thiol farnesyltransferase inhibitors: N-(4-tolylacetylamino-3-benzoylphenyl)-3-arylfurylacrylic acid amides.

Bioorg Med Chem. 2004 Sep 1;12(17):4585-600. doi: 10.1016/j.bmc.2004.07.010.

引用本文的文献

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

Pharmaceuticals (Basel). 2021 Nov 30;14(12):1249. doi: 10.3390/ph14121249.

Small Molecule Active Site Directed Tools for Studying Human Caspases.

Chem Rev. 2015 Nov 25;115(22):12546-629. doi: 10.1021/acs.chemrev.5b00434. Epub 2015 Nov 9.

Neuronal cell death in neonatal hypoxia-ischemia.

Ann Neurol. 2011 May;69(5):743-58. doi: 10.1002/ana.22419.

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

Mol Cancer Ther. 2009 May;8(5):1270-9. doi: 10.1158/1535-7163.MCT-08-0893. Epub 2009 May 5.

Targeting TNF-alpha receptors for neurotherapeutics.

Trends Neurosci. 2008 Oct;31(10):504-11. doi: 10.1016/j.tins.2008.07.005. Epub 2008 Sep 4.

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

PLoS One. 2008 May 28;3(5):e2275. doi: 10.1371/journal.pone.0002275.

文献AI研究员

20分钟写一篇综述，助力文献阅读效率提升50倍。

立即体验

用中文搜PubMed

大模型驱动的PubMed中文搜索引擎

马上搜索

文档翻译

学术文献翻译模型，支持多种主流文档格式。

立即体验