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Page 1
Potent, exceptionally selective, orally bioavailable inhibitors of TNF-alpha Converting Enzyme (TACE): novel 2-substituted-1H-benzo[d]imidazol-1-yl)methyl)benzamide P1' substituents.
Ott GR, Asakawa N, Lu Z, Anand R, Liu RQ, Covington MB, Vaddi K, Qian M, Newton RC, Christ DD, Trzaskos JM, Duan JJ. Ott GR, et al. Among authors: trzaskos jm. Bioorg Med Chem Lett. 2008 Mar 1;18(5):1577-82. doi: 10.1016/j.bmcl.2008.01.075. Epub 2008 Jan 26. Bioorg Med Chem Lett. 2008. PMID: 18242982
Pharmacokinetics and pharmacodynamics of DPC 333 ((2R)-2-((3R)-3-amino-3{4-[2-methyl-4-quinolinyl) methoxy] phenyl}-2-oxopyrrolidinyl)-N-hydroxy-4-methylpentanamide)), a potent and selective inhibitor of tumor necrosis factor alpha-converting enzyme in rodents, dogs, chimpanzees, and humans.
Qian M, Bai SA, Brogdon B, Wu JT, Liu RQ, Covington MB, Vaddi K, Newton RC, Fossler MJ, Garner CE, Deng Y, Maduskuie T, Trzaskos J, Duan JJ, Decicco CP, Christ DD. Qian M, et al. Drug Metab Dispos. 2007 Oct;35(10):1916-25. doi: 10.1124/dmd.107.015933. Epub 2007 Jul 26. Drug Metab Dispos. 2007. PMID: 17656469 Clinical Trial.
Sultam hydroxamates as novel matrix metalloproteinase inhibitors.
Cherney RJ, Mo R, Meyer DT, Hardman KD, Liu RQ, Covington MB, Qian M, Wasserman ZR, Christ DD, Trzaskos JM, Newton RC, Decicco CP. Cherney RJ, et al. Among authors: trzaskos jm. J Med Chem. 2004 Jun 3;47(12):2981-3. doi: 10.1021/jm049833g. J Med Chem. 2004. PMID: 15163180
Synthesis and structure-activity relationship of a novel, achiral series of TNF-alpha converting enzyme inhibitors.
Gilmore JL, King BW, Harris C, Maduskuie T, Mercer SE, Liu RQ, Covington MB, Qian M, Ribadeneria MD, Vaddi K, Trzaskos JM, Newton RC, Decicco CP, Duan JJ. Gilmore JL, et al. Among authors: trzaskos jm. Bioorg Med Chem Lett. 2006 May 15;16(10):2699-704. doi: 10.1016/j.bmcl.2006.02.015. Epub 2006 Mar 3. Bioorg Med Chem Lett. 2006. PMID: 16516466
A new 4-(2-methylquinolin-4-ylmethyl)phenyl P1' group for the beta-amino hydroxamic acid derived TACE inhibitors.
Chen XT, Ghavimi B, Corbett RL, Xue CB, Liu RQ, Covington MB, Qian M, Vaddi KG, Christ DD, Hartman KD, Ribadeneira MD, Trzaskos JM, Newton RC, Decicco CP, Duan JJ. Chen XT, et al. Among authors: trzaskos jm. Bioorg Med Chem Lett. 2007 Apr 1;17(7):1865-70. doi: 10.1016/j.bmcl.2007.01.041. Epub 2007 Jan 24. Bioorg Med Chem Lett. 2007. PMID: 17276676
Alpha,Beta-cyclic-beta-benzamido hydroxamic acids: Novel oxaspiro[4.4]nonane templates for the discovery of potent, selective, orally bioavailable inhibitors of tumor necrosis factor-alpha converting enzyme (TACE).
Ott GR, Asakawa N, Liu RQ, Covington MB, Qian M, Vaddi K, Newton RC, Trzaskos JM, Christ DD, Galya L, Scholz T, Marshall W, Duan JJ. Ott GR, et al. Among authors: trzaskos jm. Bioorg Med Chem Lett. 2008 Feb 15;18(4):1288-92. doi: 10.1016/j.bmcl.2008.01.030. Epub 2008 Jan 11. Bioorg Med Chem Lett. 2008. PMID: 18234496
Potent and selective aggrecanase inhibitors containing cyclic P1 substituents.
Cherney RJ, Mo R, Meyer DT, Wang L, Yao W, Wasserman ZR, Liu RQ, Covington MB, Tortorella MD, Arner EC, Qian M, Christ DD, Trzaskos JM, Newton RC, Magolda RL, Decicco CP. Cherney RJ, et al. Among authors: trzaskos jm. Bioorg Med Chem Lett. 2003 Apr 7;13(7):1297-300. doi: 10.1016/s0960-894x(03)00124-0. Bioorg Med Chem Lett. 2003. PMID: 12657268
95 results