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Page 1
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. Among authors: christ dd. 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.
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: christ dd. 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 templates for the design, synthesis, and evaluation of selective inhibitors of TNF-alpha converting enzyme (TACE).
Ott GR, Asakawa N, Lu Z, Liu RQ, Covington MB, Vaddi K, Qian M, Newton RC, Christ DD, Traskos JM, Decicco CP, Duan JJ. Ott GR, et al. Among authors: christ dd. Bioorg Med Chem Lett. 2008 Jan 15;18(2):694-9. doi: 10.1016/j.bmcl.2007.11.059. Epub 2007 Nov 21. Bioorg Med Chem Lett. 2008. PMID: 18061445
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: christ dd. 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, 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: christ dd. 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
Potent, selective, orally bioavailable inhibitors of tumor necrosis factor-alpha converting enzyme (TACE): discovery of indole, benzofuran, imidazopyridine and pyrazolopyridine P1' substituents.
Lu Z, Ott GR, Anand R, Liu RQ, Covington MB, Vaddi K, Qian M, Newton RC, Christ DD, Trzaskos J, Duan JJ. Lu Z, et al. Among authors: christ dd. Bioorg Med Chem Lett. 2008 Mar 15;18(6):1958-62. doi: 10.1016/j.bmcl.2008.01.120. Epub 2008 Feb 7. Bioorg Med Chem Lett. 2008. PMID: 18282708
Design, synthesis, and evaluation of benzothiadiazepine hydroxamates as selective tumor necrosis factor-alpha converting enzyme inhibitors.
Cherney RJ, Duan JJ, Voss ME, Chen L, Wang L, Meyer DT, Wasserman ZR, Hardman KD, Liu RQ, Covington MB, Qian M, Mandlekar S, Christ DD, Trzaskos JM, Newton RC, Magolda RL, Wexler RR, Decicco CP. Cherney RJ, et al. Among authors: christ dd. J Med Chem. 2003 May 8;46(10):1811-23. doi: 10.1021/jm020475w. J Med Chem. 2003. PMID: 12723945
Rational design, synthesis and structure-activity relationships of a cyclic succinate series of TNF-alpha converting enzyme inhibitors. Part 2: lead optimization.
Xue CB, He X, Roderick J, Corbett RL, Duan JJ, Liu RQ, Covington MB, Qian M, Ribadeneira MD, Vaddi K, Christ DD, Newton RC, Trzaskos JM, Magolda RL, Wexler RR, Decicco CP. Xue CB, et al. Among authors: christ dd. Bioorg Med Chem Lett. 2003 Dec 15;13(24):4299-304. doi: 10.1016/j.bmcl.2003.09.057. Bioorg Med Chem Lett. 2003. PMID: 14643313
74 results