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Page 1
MMP-13 selective alpha-sulfone hydroxamates: identification of selective P1' amides.
Fobian YM, Freskos JN, Barta TE, Bedell LJ, Heintz R, Kassab DJ, Kiefer JR, Mischke BV, Molyneaux JM, Mullins P, Munie GE, Becker DP. Fobian YM, et al. Among authors: kiefer jr. Bioorg Med Chem Lett. 2011 May 15;21(10):2823-5. doi: 10.1016/j.bmcl.2011.03.095. Epub 2011 Apr 1. Bioorg Med Chem Lett. 2011. PMID: 21493063
Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.
Becker DP, Barta TE, Bedell LJ, Boehm TL, Bond BR, Carroll J, Carron CP, Decrescenzo GA, Easton AM, Freskos JN, Funckes-Shippy CL, Heron M, Hockerman S, Howard CP, Kiefer JR, Li MH, Mathis KJ, McDonald JJ, Mehta PP, Munie GE, Sunyer T, Swearingen CA, Villamil CI, Welsch D, Williams JM, Yu Y, Yao J. Becker DP, et al. Among authors: kiefer jr. J Med Chem. 2010 Sep 23;53(18):6653-80. doi: 10.1021/jm100669j. J Med Chem. 2010. PMID: 20726512
Structure analysis reveals the flexibility of the ADAMTS-5 active site.
Shieh HS, Tomasselli AG, Mathis KJ, Schnute ME, Woodard SS, Caspers N, Williams JM, Kiefer JR, Munie G, Wittwer A, Malfait AM, Tortorella MD. Shieh HS, et al. Among authors: kiefer jr. Protein Sci. 2011 Apr;20(4):735-44. doi: 10.1002/pro.606. Protein Sci. 2011. PMID: 21370305 Free PMC article.
2-(6-Phenyl-1H-indazol-3-yl)-1H-benzo[d]imidazoles: design and synthesis of a potent and isoform selective PKC-zeta inhibitor.
Trujillo JI, Kiefer JR, Huang W, Thorarensen A, Xing L, Caspers NL, Day JE, Mathis KJ, Kretzmer KK, Reitz BA, Weinberg RA, Stegeman RA, Wrightstone A, Christine L, Compton R, Li X. Trujillo JI, et al. Among authors: kiefer jr. Bioorg Med Chem Lett. 2009 Feb 1;19(3):908-11. doi: 10.1016/j.bmcl.2008.11.105. Epub 2008 Dec 6. Bioorg Med Chem Lett. 2009. PMID: 19097791
The novel benzopyran class of selective cyclooxygenase-2 inhibitors. Part 2: the second clinical candidate having a shorter and favorable human half-life.
Wang JL, Limburg D, Graneto MJ, Springer J, Hamper JR, Liao S, Pawlitz JL, Kurumbail RG, Maziasz T, Talley JJ, Kiefer JR, Carter J. Wang JL, et al. Among authors: kiefer jr. Bioorg Med Chem Lett. 2010 Dec 1;20(23):7159-63. doi: 10.1016/j.bmcl.2010.07.054. Epub 2010 Jul 24. Bioorg Med Chem Lett. 2010. PMID: 20709553
Investigation of the binding pocket of human hematopoietic prostaglandin (PG) D2 synthase (hH-PGDS): a tale of two waters.
Trujillo JI, Kiefer JR, Huang W, Day JE, Moon J, Jerome GM, Bono CP, Kornmeier CM, Williams ML, Kuhn C, Rennie GR, Wynn TA, Carron CP, Thorarensen A. Trujillo JI, et al. Among authors: kiefer jr. Bioorg Med Chem Lett. 2012 Jun 1;22(11):3795-9. doi: 10.1016/j.bmcl.2012.04.004. Epub 2012 Apr 13. Bioorg Med Chem Lett. 2012. PMID: 22546671
Discovery of an Oral Potent Selective Inhibitor of Hematopoietic Prostaglandin D Synthase (HPGDS).
Carron CP, Trujillo JI, Olson KL, Huang W, Hamper BC, Dice T, Neal BE, Pelc MJ, Day JE, Rohrer DC, Kiefer JR, Moon JB, Schweitzer BA, Blake TD, Turner SR, Woerndle R, Case BL, Bono CP, Dilworth VM, Funckes-Shippy CL, Hood BL, Jerome GM, Kornmeier CM, Radabaugh MR, Williams ML, Davies MS, Wegner CD, Welsch DJ, Abraham WM, Warren CJ, Dowty ME, Hua F, Zutshi A, Yang JZ, Thorarensen A. Carron CP, et al. Among authors: kiefer jr. ACS Med Chem Lett. 2010 Feb 2;1(2):59-63. doi: 10.1021/ml900025z. eCollection 2010 May 13. ACS Med Chem Lett. 2010. PMID: 24900177 Free PMC article.
A reversed sulfonamide series of selective RORc inverse agonists.
van Niel MB, Fauber BP, Cartwright M, Gaines S, Killen JC, René O, Ward SI, de Leon Boenig G, Deng Y, Eidenschenk C, Everett C, Gancia E, Ganguli A, Gobbi A, Hawkins J, Johnson AR, Kiefer JR, La H, Lockey P, Norman M, Ouyang W, Qin A, Wakes N, Waszkowycz B, Wong H. van Niel MB, et al. Among authors: kiefer jr. Bioorg Med Chem Lett. 2014 Dec 15;24(24):5769-5776. doi: 10.1016/j.bmcl.2014.10.037. Epub 2014 Oct 25. Bioorg Med Chem Lett. 2014. PMID: 25453817
67 results