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Page 1
Pyrrolo[1,2-f]triazines as JAK2 inhibitors: achieving potency and selectivity for JAK2 over JAK3.
Harikrishnan LS, Kamau MG, Wan H, Inghrim JA, Zimmermann K, Sang X, Mastalerz HA, Johnson WL, Zhang G, Lombardo LJ, Poss MA, Trainor GL, Tokarski JS, Lorenzi MV, You D, Gottardis MM, Baldwin KF, Lippy J, Nirschl DS, Qiu R, Miller AV, Khan J, Sack JS, Purandare AV. Harikrishnan LS, et al. Among authors: trainor gl. Bioorg Med Chem Lett. 2011 Mar 1;21(5):1425-8. doi: 10.1016/j.bmcl.2011.01.022. Epub 2011 Jan 11. Bioorg Med Chem Lett. 2011. PMID: 21282055
Discovery of a 2,4-disubstituted pyrrolo[1,2-f][1,2,4]triazine inhibitor (BMS-754807) of insulin-like growth factor receptor (IGF-1R) kinase in clinical development.
Wittman MD, Carboni JM, Yang Z, Lee FY, Antman M, Attar R, Balimane P, Chang C, Chen C, Discenza L, Frennesson D, Gottardis MM, Greer A, Hurlburt W, Johnson W, Langley DR, Li A, Li J, Liu P, Mastalerz H, Mathur A, Menard K, Patel K, Sack J, Sang X, Saulnier M, Smith D, Stefanski K, Trainor G, Velaparthi U, Zhang G, Zimmermann K, Vyas DM. Wittman MD, et al. J Med Chem. 2009 Dec 10;52(23):7360-3. doi: 10.1021/jm900786r. J Med Chem. 2009. PMID: 19778024
Discovery of pyrrolopyridine-pyridone based inhibitors of Met kinase: synthesis, X-ray crystallographic analysis, and biological activities.
Kim KS, Zhang L, Schmidt R, Cai ZW, Wei D, Williams DK, Lombardo LJ, Trainor GL, Xie D, Zhang Y, An Y, Sack JS, Tokarski JS, Darienzo C, Kamath A, Marathe P, Zhang Y, Lippy J, Jeyaseelan R Sr, Wautlet B, Henley B, Gullo-Brown J, Manne V, Hunt JT, Fargnoli J, Borzilleri RM. Kim KS, et al. Among authors: trainor gl. J Med Chem. 2008 Sep 11;51(17):5330-41. doi: 10.1021/jm800476q. Epub 2008 Aug 9. J Med Chem. 2008. PMID: 18690676
Optimization of pyrazole inhibitors of Coactivator Associated Arginine Methyltransferase 1 (CARM1).
Huynh T, Chen Z, Pang S, Geng J, Bandiera T, Bindi S, Vianello P, Roletto F, Thieffine S, Galvani A, Vaccaro W, Poss MA, Trainor GL, Lorenzi MV, Gottardis M, Jayaraman L, Purandare AV. Huynh T, et al. Among authors: trainor gl. Bioorg Med Chem Lett. 2009 Jun 1;19(11):2924-7. doi: 10.1016/j.bmcl.2009.04.075. Epub 2009 Apr 22. Bioorg Med Chem Lett. 2009. PMID: 19419866
Design, synthesis and structure-activity relationships of novel biarylamine-based Met kinase inhibitors.
Williams DK, Chen XT, Tarby C, Kaltenbach R, Cai ZW, Tokarski JS, An Y, Sack JS, Wautlet B, Gullo-Brown J, Henley BJ, Jeyaseelan R, Kellar K, Manne V, Trainor GL, Lombardo LJ, Fargnoli J, Borzilleri RM. Williams DK, et al. Among authors: trainor gl. Bioorg Med Chem Lett. 2010 May 1;20(9):2998-3002. doi: 10.1016/j.bmcl.2010.01.042. Epub 2010 Jan 20. Bioorg Med Chem Lett. 2010. PMID: 20382527
Identification and optimization of small molecule antagonists of vasoactive intestinal peptide receptor-1 (VIPR1).
Harikrishnan LS, Srivastava N, Kayser LE, Nirschl DS, Kumaragurubaran K, Roy A, Gupta A, Karmakar S, Karatt T, Mathur A, Burford NT, Chen J, Kong Y, Cvijic M, Cooper CB, Poss MA, Trainor GL, Wong TW. Harikrishnan LS, et al. Among authors: trainor gl. Bioorg Med Chem Lett. 2012 Mar 15;22(6):2287-90. doi: 10.1016/j.bmcl.2012.01.082. Epub 2012 Feb 2. Bioorg Med Chem Lett. 2012. PMID: 22365758 Free article.
Modulation of cofilin phosphorylation by inhibition of the Lim family kinases.
He L, Seitz SP, Trainor GL, Tortolani D, Vaccaro W, Poss M, Tarby CM, Tokarski JS, Penhallow B, Hung CY, Attar R, Lin TA. He L, et al. Among authors: trainor gl. Bioorg Med Chem Lett. 2012 Sep 15;22(18):5995-8. doi: 10.1016/j.bmcl.2012.07.002. Epub 2012 Jul 21. Bioorg Med Chem Lett. 2012. PMID: 22902653
9H-Carbazole-1-carboxamides as potent and selective JAK2 inhibitors.
Zimmermann K, Sang X, Mastalerz HA, Johnson WL, Zhang G, Liu Q, Batt D, Lombardo LJ, Vyas D, Trainor GL, Tokarski JS, Lorenzi MV, You D, Gottardis MM, Lippy J, Khan J, Sack JS, Purandare AV. Zimmermann K, et al. Among authors: trainor gl. Bioorg Med Chem Lett. 2015 Jul 15;25(14):2809-12. doi: 10.1016/j.bmcl.2015.04.101. Epub 2015 May 11. Bioorg Med Chem Lett. 2015. PMID: 25987372
86 results