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Page 1
5-amino-pyrazoles as potent and selective p38α inhibitors.
Das J, Moquin RV, Dyckman AJ, Li T, Pitt S, Zhang R, Shen DR, McIntyre KW, Gillooly K, Doweyko AM, Newitt JA, Sack JS, Zhang H, Kiefer SE, Kish K, McKinnon M, Barrish JC, Dodd JH, Schieven GL, Leftheris K. Das J, et al. Among authors: sack js. Bioorg Med Chem Lett. 2010 Dec 1;20(23):6886-9. doi: 10.1016/j.bmcl.2010.10.034. Epub 2010 Oct 13. Bioorg Med Chem Lett. 2010. PMID: 21035336
Discovery of potent and selective nonsteroidal indazolyl amide glucocorticoid receptor agonists.
Sheppeck JE 2nd, Gilmore JL, Xiao HY, Dhar TG, Nirschl D, Doweyko AM, Sack JS, Corbett MJ, Malley MF, Gougoutas JZ, Mckay L, Cunningham MD, Habte SF, Dodd JH, Nadler SG, Somerville JE, Barrish JC. Sheppeck JE 2nd, et al. Among authors: sack js. Bioorg Med Chem Lett. 2013 Oct 1;23(19):5442-7. doi: 10.1016/j.bmcl.2013.06.089. Epub 2013 Jul 9. Bioorg Med Chem Lett. 2013. PMID: 23953070
The discovery of orally active triaminotriazine aniline amides as inhibitors of p38 MAP kinase.
Leftheris K, Ahmed G, Chan R, Dyckman AJ, Hussain Z, Ho K, Hynes J Jr, Letourneau J, Li W, Lin S, Metzger A, Moriarty KJ, Riviello C, Shimshock Y, Wen J, Wityak J, Wrobleski ST, Wu H, Wu J, Desai M, Gillooly KM, Lin TH, Loo D, McIntyre KW, Pitt S, Shen DR, Shuster DJ, Zhang R, Diller D, Doweyko A, Sack J, Baldwin J, Barrish J, Dodd J, Henderson I, Kanner S, Schieven GL, Webb M. Leftheris K, et al. J Med Chem. 2004 Dec 2;47(25):6283-91. doi: 10.1021/jm049521d. J Med Chem. 2004. PMID: 15566298
Molecular design and structure--activity relationships leading to the potent, selective, and orally active thrombin active site inhibitor BMS-189664.
Das J, Kimball SD, Hall SE, Han WC, Iwanowicz E, Lin J, Moquin RV, Reid JA, Sack JS, Malley MF, Chang CY, Chong S, Wang-Iverson DB, Roberts DG, Seiler SM, Schumacher WA, Ogletree ML. Das J, et al. Among authors: sack js. Bioorg Med Chem Lett. 2002 Jan 7;12(1):45-9. doi: 10.1016/s0960-894x(01)00667-9. Bioorg Med Chem Lett. 2002. PMID: 11738570
Synthesis and SAR of p38alpha MAP kinase inhibitors based on heterobicyclic scaffolds.
Murali Dhar TG, Wrobleski ST, Lin S, Furch JA, Nirschl DS, Fan Y, Todderud G, Pitt S, Doweyko AM, Sack JS, Mathur A, McKinnon M, Barrish JC, Dodd JH, Schieven GL, Leftheris K. Murali Dhar TG, et al. Among authors: sack js. Bioorg Med Chem Lett. 2007 Sep 15;17(18):5019-24. doi: 10.1016/j.bmcl.2007.07.029. Epub 2007 Jul 21. Bioorg Med Chem Lett. 2007. PMID: 17664068
Design, synthesis, and anti-inflammatory properties of orally active 4-(phenylamino)-pyrrolo[2,1-f][1,2,4]triazine p38alpha mitogen-activated protein kinase inhibitors.
Hynes J Jr, Dyckman AJ, Lin S, Wrobleski ST, Wu H, Gillooly KM, Kanner SB, Lonial H, Loo D, McIntyre KW, Pitt S, Shen DR, Shuster DJ, Yang X, Zhang R, Behnia K, Zhang H, Marathe PH, Doweyko AM, Tokarski JS, Sack JS, Pokross M, Kiefer SE, Newitt JA, Barrish JC, Dodd J, Schieven GL, Leftheris K. Hynes J Jr, et al. Among authors: sack js. J Med Chem. 2008 Jan 10;51(1):4-16. doi: 10.1021/jm7009414. Epub 2007 Dec 12. J Med Chem. 2008. PMID: 18072718
Benzothiazole based inhibitors of p38alpha MAP kinase.
Liu C, Lin J, Pitt S, Zhang RF, Sack JS, Kiefer SE, Kish K, Doweyko AM, Zhang H, Marathe PH, Trzaskos J, Mckinnon M, Dodd JH, Barrish JC, Schieven GL, Leftheris K. Liu C, et al. Among authors: sack js. Bioorg Med Chem Lett. 2008 Mar 15;18(6):1874-9. doi: 10.1016/j.bmcl.2008.02.011. Epub 2008 Feb 10. Bioorg Med Chem Lett. 2008. PMID: 18296051
The discovery of (R)-2-(sec-butylamino)-N-(2-methyl-5-(methylcarbamoyl)phenyl) thiazole-5-carboxamide (BMS-640994)-A potent and efficacious p38alpha MAP kinase inhibitor.
Hynes J Jr, Wu H, Pitt S, Shen DR, Zhang R, Schieven GL, Gillooly KM, Shuster DJ, Taylor TL, Yang X, McIntyre KW, McKinnon M, Zhang H, Marathe PH, Doweyko AM, Kish K, Kiefer SE, Sack JS, Newitt JA, Barrish JC, Dodd J, Leftheris K. Hynes J Jr, et al. Among authors: sack js. Bioorg Med Chem Lett. 2008 Mar 15;18(6):1762-7. doi: 10.1016/j.bmcl.2008.02.031. Epub 2008 Feb 16. Bioorg Med Chem Lett. 2008. PMID: 18313298
Synthesis and SAR of new pyrrolo[2,1-f][1,2,4]triazines as potent p38 alpha MAP kinase inhibitors.
Wrobleski ST, Lin S, Hynes J Jr, Wu H, Pitt S, Shen DR, Zhang R, Gillooly KM, Shuster DJ, McIntyre KW, Doweyko AM, Kish KF, Tredup JA, Duke GJ, Sack JS, McKinnon M, Dodd J, Barrish JC, Schieven GL, Leftheris K. Wrobleski ST, et al. Among authors: sack js. Bioorg Med Chem Lett. 2008 Apr 15;18(8):2739-44. doi: 10.1016/j.bmcl.2008.02.067. Epub 2008 Mar 4. Bioorg Med Chem Lett. 2008. PMID: 18364256
116 results