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Page 1
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
Inhibitors of human mitotic kinesin Eg5: characterization of the 4-phenyl-tetrahydroisoquinoline lead series.
Tarby CM, Kaltenbach RF 3rd, Huynh T, Pudzianowski A, Shen H, Ortega-Nanos M, Sheriff S, Newitt JA, McDonnell PA, Burford N, Fairchild CR, Vaccaro W, Chen Z, Borzilleri RM, Naglich J, Lombardo LJ, Gottardis M, Trainor GL, Roussell DL. Tarby CM, et al. Among authors: trainor gl. Bioorg Med Chem Lett. 2006 Apr 15;16(8):2095-100. doi: 10.1016/j.bmcl.2006.01.056. Epub 2006 Feb 3. Bioorg Med Chem Lett. 2006. PMID: 16458511
Discovery and preclinical studies of 5-isopropyl-6-(5-methyl-1,3,4-oxadiazol-2-yl)-N-(2-methyl-1H-pyrrolo[2,3-b]pyridin-5-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amine (BMS-645737), an in vivo active potent VEGFR-2 inhibitor.
Ruel R, Thibeault C, L'Heureux A, Martel A, Cai ZW, Wei D, Qian L, Barrish JC, Mathur A, D'Arienzo C, Hunt JT, Kamath A, Marathe P, Zhang Y, Derbin G, Wautlet B, Mortillo S, Jeyaseelan R Sr, Henley B, Tejwani R, Bhide RS, Trainor GL, Fargnoli J, Lombardo LJ. Ruel R, et al. Among authors: trainor gl. Bioorg Med Chem Lett. 2008 May 1;18(9):2985-9. doi: 10.1016/j.bmcl.2008.03.057. Epub 2008 Mar 22. Bioorg Med Chem Lett. 2008. PMID: 18395443
Discovery of N-(4-(2-amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide (BMS-777607), a selective and orally efficacious inhibitor of the Met kinase superfamily.
Schroeder GM, An Y, Cai ZW, Chen XT, Clark C, Cornelius LA, Dai J, Gullo-Brown J, Gupta A, Henley B, Hunt JT, Jeyaseelan R, Kamath A, Kim K, Lippy J, Lombardo LJ, Manne V, Oppenheimer S, Sack JS, Schmidt RJ, Shen G, Stefanski K, Tokarski JS, Trainor GL, Wautlet BS, Wei D, Williams DK, Zhang Y, Zhang Y, Fargnoli J, Borzilleri RM. Schroeder GM, et al. Among authors: trainor gl. J Med Chem. 2009 Mar 12;52(5):1251-4. doi: 10.1021/jm801586s. J Med Chem. 2009. PMID: 19260711
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
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
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
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
BMS-871: a novel orally active pan-Notch inhibitor as an anticancer agent.
Shan W, Balog A, Quesnelle C, Gill P, Han WC, Norris D, Mandal S, Thiruvenkadam R, Gona KB, Thiyagarajan K, Kandula S, McGlinchey K, Menard K, Wen ML, Rose A, White R, Guarino V, Shen DR, Cvijic ME, Ranasinghe A, Dai J, Zhang Y, Wu DR, Mathur A, Rampulla R, Trainor G, Hunt JT, Vite GD, Westhouse R, Lee FY, Gavai AV. Shan W, et al. Bioorg Med Chem Lett. 2015 May 1;25(9):1905-9. doi: 10.1016/j.bmcl.2015.03.038. Epub 2015 Mar 23. Bioorg Med Chem Lett. 2015. PMID: 25857941
86 results