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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: wautlet b. J Med Chem. 2008 Sep 11;51(17):5330-41. doi: 10.1021/jm800476q. Epub 2008 Aug 9. J Med Chem. 2008. PMID: 18690676
Design, synthesis, and evaluation of orally active 4-(2,4-difluoro-5-(methoxycarbamoyl)phenylamino)pyrrolo[2,1-f][1,2,4]triazines as dual vascular endothelial growth factor receptor-2 and fibroblast growth factor receptor-1 inhibitors.
Borzilleri RM, Zheng X, Qian L, Ellis C, Cai ZW, Wautlet BS, Mortillo S, Jeyaseelan R Sr, Kukral DW, Fura A, Kamath A, Vyas V, Tokarski JS, Barrish JC, Hunt JT, Lombardo LJ, Fargnoli J, Bhide RS. Borzilleri RM, et al. J Med Chem. 2005 Jun 16;48(12):3991-4008. doi: 10.1021/jm0501275. J Med Chem. 2005. PMID: 15943473
Discovery and evaluation of N-cyclopropyl- 2,4-difluoro-5-((2-(pyridin-2-ylamino)thiazol-5- ylmethyl)amino)benzamide (BMS-605541), a selective and orally efficacious inhibitor of vascular endothelial growth factor receptor-2.
Borzilleri RM, Bhide RS, Barrish JC, D'Arienzo CJ, Derbin GM, Fargnoli J, Hunt JT, Jeyaseelan R Sr, Kamath A, Kukral DW, Marathe P, Mortillo S, Qian L, Tokarski JS, Wautlet BS, Zheng X, Lombardo LJ. Borzilleri RM, et al. J Med Chem. 2006 Jun 29;49(13):3766-9. doi: 10.1021/jm060347y. J Med Chem. 2006. PMID: 16789733
Discovery of brivanib alaninate ((S)-((R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan-2-yl)2-aminopropanoate), a novel prodrug of dual vascular endothelial growth factor receptor-2 and fibroblast growth factor receptor-1 kinase inhibitor (BMS-540215).
Cai ZW, Zhang Y, Borzilleri RM, Qian L, Barbosa S, Wei D, Zheng X, Wu L, Fan J, Shi Z, Wautlet BS, Mortillo S, Jeyaseelan R Sr, Kukral DW, Kamath A, Marathe P, D'Arienzo C, Derbin G, Barrish JC, Robl JA, Hunt JT, Lombardo LJ, Fargnoli J, Bhide RS. Cai ZW, et al. Among authors: wautlet bs. J Med Chem. 2008 Mar 27;51(6):1976-80. doi: 10.1021/jm7013309. Epub 2008 Feb 21. J Med Chem. 2008. PMID: 18288793
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: wautlet bs. J Med Chem. 2009 Mar 12;52(5):1251-4. doi: 10.1021/jm801586s. J Med Chem. 2009. PMID: 19260711
Discovery and preclinical studies of (R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5- methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan- 2-ol (BMS-540215), an in vivo active potent VEGFR-2 inhibitor.
Bhide RS, Cai ZW, Zhang YZ, Qian L, Wei D, Barbosa S, Lombardo LJ, Borzilleri RM, Zheng X, Wu LI, Barrish JC, Kim SH, Leavitt K, Mathur A, Leith L, Chao S, Wautlet B, Mortillo S, Jeyaseelan R Sr, Kukral D, Hunt JT, Kamath A, Fura A, Vyas V, Marathe P, D'Arienzo C, Derbin G, Fargnoli J. Bhide RS, et al. Among authors: wautlet b. J Med Chem. 2006 Apr 6;49(7):2143-6. doi: 10.1021/jm051106d. J Med Chem. 2006. PMID: 16570908
Synthesis, SAR, and Evaluation of 4-[2,4-Difluoro-5-(cyclopropylcarbamoyl)phenylamino]pyrrolo[2,1-f][1,2,4]triazine-based VEGFR-2 kinase inhibitors.
Cai ZW, Wei D, Borzilleri RM, Qian L, Kamath A, Mortillo S, Wautlet B, Henley BJ, Jeyaseelan R Sr, Tokarski J, Hunt JT, Bhide RS, Fargnoli J, Lombardo LJ. Cai ZW, et al. Among authors: wautlet b. Bioorg Med Chem Lett. 2008 Feb 15;18(4):1354-8. doi: 10.1016/j.bmcl.2008.01.012. Epub 2008 Jan 9. Bioorg Med Chem Lett. 2008. PMID: 18221875
Identification of pyrrolo[2,1-f][1,2,4]triazine-based inhibitors of Met kinase.
Schroeder GM, Chen XT, Williams DK, Nirschl DS, Cai ZW, Wei D, Tokarski JS, An Y, Sack J, Chen Z, Huynh T, Vaccaro W, Poss M, Wautlet B, Gullo-Brown J, Kellar K, Manne V, Hunt JT, Wong TW, Lombardo LJ, Fargnoli J, Borzilleri RM. Schroeder GM, et al. Among authors: wautlet b. Bioorg Med Chem Lett. 2008 Mar 15;18(6):1945-51. doi: 10.1016/j.bmcl.2008.01.121. Epub 2008 Feb 7. Bioorg Med Chem Lett. 2008. PMID: 18289854
19 results