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3-Amido pyrrolopyrazine JAK kinase inhibitors: development of a JAK3 vs JAK1 selective inhibitor and evaluation in cellular and in vivo models.
Soth M, Hermann JC, Yee C, Alam M, Barnett JW, Berry P, Browner MF, Frank K, Frauchiger S, Harris S, He Y, Hekmat-Nejad M, Hendricks T, Henningsen R, Hilgenkamp R, Ho H, Hoffman A, Hsu PY, Hu DQ, Itano A, Jaime-Figueroa S, Jahangir A, Jin S, Kuglstatter A, Kutach AK, Liao C, Lynch S, Menke J, Niu L, Patel V, Railkar A, Roy D, Shao A, Shaw D, Steiner S, Sun Y, Tan SL, Wang S, Vu MD. Soth M, et al. Among authors: hermann jc. J Med Chem. 2013 Jan 10;56(1):345-56. doi: 10.1021/jm301646k. Epub 2012 Dec 19. J Med Chem. 2013. PMID: 23214979
Pyrrolopyrazines as selective spleen tyrosine kinase inhibitors.
Padilla F, Bhagirath N, Chen S, Chiao E, Goldstein DM, Hermann JC, Hsu J, Kennedy-Smith JJ, Kuglstatter A, Liao C, Liu W, Lowrie LE Jr, Luk KC, Lynch SM, Menke J, Niu L, Owens TD, O-Yang C, Railkar A, Schoenfeld RC, Slade M, Steiner S, Tan YC, Villaseñor AG, Wang C, Wanner J, Xie W, Xu D, Zhang X, Zhou M, Lucas MC. Padilla F, et al. Among authors: hermann jc. J Med Chem. 2013 Feb 28;56(4):1677-92. doi: 10.1021/jm301720p. Epub 2013 Feb 12. J Med Chem. 2013. PMID: 23350847
Development of amino-pyrimidine inhibitors of c-Jun N-terminal kinase (JNK): kinase profiling guided optimization of a 1,2,3-benzotriazole lead.
Palmer WS, Alam M, Arzeno HB, Chang KC, Dunn JP, Goldstein DM, Gong L, Goyal B, Hermann JC, Hogg JH, Hsieh G, Jahangir A, Janson C, Jin S, Ursula Kammlott R, Kuglstatter A, Lukacs C, Michoud C, Niu L, Reuter DC, Shao A, Silva T, Trejo-Martin TA, Stein K, Tan YC, Tivitmahaisoon P, Tran P, Wagner P, Weller P, Wu SY. Palmer WS, et al. Among authors: hermann jc. Bioorg Med Chem Lett. 2013 Mar 1;23(5):1486-92. doi: 10.1016/j.bmcl.2012.12.047. Epub 2012 Dec 22. Bioorg Med Chem Lett. 2013. PMID: 23352510
Strategic use of conformational bias and structure based design to identify potent JAK3 inhibitors with improved selectivity against the JAK family and the kinome.
Lynch SM, DeVicente J, Hermann JC, Jaime-Figueroa S, Jin S, Kuglstatter A, Li H, Lovey A, Menke J, Niu L, Patel V, Roy D, Soth M, Steiner S, Tivitmahaisoon P, Vu MD, Yee C. Lynch SM, et al. Among authors: hermann jc. Bioorg Med Chem Lett. 2013 May 1;23(9):2793-800. doi: 10.1016/j.bmcl.2013.02.012. Epub 2013 Feb 13. Bioorg Med Chem Lett. 2013. PMID: 23540648
Using ovality to predict nonmutagenic, orally efficacious pyridazine amides as cell specific spleen tyrosine kinase inhibitors.
Lucas MC, Bhagirath N, Chiao E, Goldstein DM, Hermann JC, Hsu PY, Kirchner S, Kennedy-Smith JJ, Kuglstatter A, Lukacs C, Menke J, Niu L, Padilla F, Peng Y, Polonchuk L, Railkar A, Slade M, Soth M, Xu D, Yadava P, Yee C, Zhou M, Liao C. Lucas MC, et al. Among authors: hermann jc. J Med Chem. 2014 Mar 27;57(6):2683-91. doi: 10.1021/jm401982j. Epub 2014 Feb 26. J Med Chem. 2014. PMID: 24520947
Scaffold hopping towards potent and selective JAK3 inhibitors: discovery of novel C-5 substituted pyrrolopyrazines.
de Vicente J, Lemoine R, Bartlett M, Hermann JC, Hekmat-Nejad M, Henningsen R, Jin S, Kuglstatter A, Li H, Lovey AJ, Menke J, Niu L, Patel V, Petersen A, Setti L, Shao A, Tivitmahaisoon P, Vu MD, Soth M. de Vicente J, et al. Among authors: hermann jc. Bioorg Med Chem Lett. 2014 Nov 1;24(21):4969-75. doi: 10.1016/j.bmcl.2014.09.031. Epub 2014 Sep 21. Bioorg Med Chem Lett. 2014. PMID: 25262541
Rational design of highly selective spleen tyrosine kinase inhibitors.
Lucas MC, Goldstein DM, Hermann JC, Kuglstatter A, Liu W, Luk KC, Padilla F, Slade M, Villaseñor AG, Wanner J, Xie W, Zhang X, Liao C. Lucas MC, et al. Among authors: hermann jc. J Med Chem. 2012 Dec 13;55(23):10414-23. doi: 10.1021/jm301367c. Epub 2012 Nov 27. J Med Chem. 2012. PMID: 23151054
Metal impurities cause false positives in high-throughput screening campaigns.
Hermann JC, Chen Y, Wartchow C, Menke J, Gao L, Gleason SK, Haynes NE, Scott N, Petersen A, Gabriel S, Vu B, George KM, Narayanan A, Li SH, Qian H, Beatini N, Niu L, Gan QF. Hermann JC, et al. ACS Med Chem Lett. 2012 Dec 12;4(2):197-200. doi: 10.1021/ml3003296. eCollection 2013 Feb 14. ACS Med Chem Lett. 2012. PMID: 24900642 Free PMC article.
Fragment-Based Drug Design of Novel Pyranopyridones as Cell Active and Orally Bioavailable Tankyrase Inhibitors.
de Vicente J, Tivitmahaisoon P, Berry P, Bolin DR, Carvajal D, He W, Huang KS, Janson C, Liang L, Lukacs C, Petersen A, Qian H, Yi L, Zhuang Y, Hermann JC. de Vicente J, et al. Among authors: hermann jc. ACS Med Chem Lett. 2015 Aug 4;6(9):1019-24. doi: 10.1021/acsmedchemlett.5b00251. eCollection 2015 Sep 10. ACS Med Chem Lett. 2015. PMID: 26396691 Free PMC article.
657 results