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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. Among authors: fura a. J Med Chem. 2005 Jun 16;48(12):3991-4008. doi: 10.1021/jm0501275. J Med Chem. 2005. PMID: 15943473
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: fura a. J Med Chem. 2006 Apr 6;49(7):2143-6. doi: 10.1021/jm051106d. J Med Chem. 2006. PMID: 16570908
Discovery of potent, orally-active, and muscle-selective androgen receptor modulators based on an N-aryl-hydroxybicyclohydantoin scaffold.
Sun C, Robl JA, Wang TC, Huang Y, Kuhns JE, Lupisella JA, Beehler BC, Golla R, Sleph PG, Seethala R, Fura A, Krystek SR Jr, An Y, Malley MF, Sack JS, Salvati ME, Grover GJ, Ostrowski J, Hamann LG. Sun C, et al. Among authors: fura a. J Med Chem. 2006 Dec 28;49(26):7596-9. doi: 10.1021/jm061101w. J Med Chem. 2006. PMID: 17181141
Tandem optimization of target activity and elimination of mutagenic potential in a potent series of N-aryl bicyclic hydantoin-based selective androgen receptor modulators.
Hamann LG, Manfredi MC, Sun C, Krystek SR Jr, Huang Y, Bi Y, Augeri DJ, Wang T, Zou Y, Betebenner DA, Fura A, Seethala R, Golla R, Kuhns JE, Lupisella JA, Darienzo CJ, Custer LL, Price JL, Johnson JM, Biller SA, Zahler R, Ostrowski J. Hamann LG, et al. Among authors: fura a. Bioorg Med Chem Lett. 2007 Apr 1;17(7):1860-4. doi: 10.1016/j.bmcl.2007.01.076. Epub 2007 Jan 27. Bioorg Med Chem Lett. 2007. PMID: 17292608
Discovery of potent and muscle selective androgen receptor modulators through scaffold modifications.
Li JJ, Sutton JC, Nirschl A, Zou Y, Wang H, Sun C, Pi Z, Johnson R, Krystek SR Jr, Seethala R, Golla R, Sleph PG, Beehler BC, Grover GJ, Fura A, Vyas VP, Li CY, Gougoutas JZ, Galella MA, Zahler R, Ostrowski J, Hamann LG. Li JJ, et al. Among authors: fura a. J Med Chem. 2007 Jun 28;50(13):3015-25. doi: 10.1021/jm070312d. Epub 2007 Jun 7. J Med Chem. 2007. PMID: 17552509
Identification and optimization of a novel series of [2.2.1]-oxabicyclo imide-based androgen receptor antagonists.
Salvati ME, Balog A, Shan W, Rampulla R, Giese S, Mitt T, Furch JA, Vite GD, Attar RM, Jure-Kunkel M, Geng J, Rizzo CA, Gottardis MM, Krystek SR, Gougoutas J, Galella MA, Obermeier M, Fura A, Chandrasena G. Salvati ME, et al. Among authors: fura a. Bioorg Med Chem Lett. 2008 Mar 15;18(6):1910-5. doi: 10.1016/j.bmcl.2008.02.006. Epub 2008 Feb 8. Bioorg Med Chem Lett. 2008. PMID: 18291644
47 results