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Page 1
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: bhide rs. 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
Development of highly potent inhibitors of Ras farnesyltransferase possessing cellular and in vivo activity.
Leftheris K, Kline T, Vite GD, Cho YH, Bhide RS, Patel DV, Patel MM, Schmidt RJ, Weller HN, Andahazy ML, Carboni JM, Gullo-Brown JL, Lee FY, Ricca C, Rose WC, Yan N, Barbacid M, Hunt JT, Meyers CA, Seizinger BR, Zahler R, Manne V. Leftheris K, et al. Among authors: bhide rs. J Med Chem. 1996 Jan 5;39(1):224-36. doi: 10.1021/jm950642a. J Med Chem. 1996. PMID: 8568812
Discovery and structure-activity relationships of imidazole-containing tetrahydrobenzodiazepine inhibitors of farnesyltransferase.
Ding CZ, Batorsky R, Bhide R, Chao HJ, Cho Y, Chong S, Gullo-Brown J, Guo P, Kim SH, Lee F, Leftheris K, Miller A, Mitt T, Patel M, Penhallow BA, Ricca C, Rose WC, Schmidt R, Slusarchyk WA, Vite G, Yan N, Manne V, Hunt JT. Ding CZ, et al. J Med Chem. 1999 Dec 16;42(25):5241-53. doi: 10.1021/jm990391w. J Med Chem. 1999. PMID: 10602709
Discovery of (R)-7-cyano-2,3,4, 5-tetrahydro-1-(1H-imidazol-4-ylmethyl)-3- (phenylmethyl)-4-(2-thienylsulfonyl)-1H-1,4-benzodiazepine (BMS-214662), a farnesyltransferase inhibitor with potent preclinical antitumor activity.
Hunt JT, Ding CZ, Batorsky R, Bednarz M, Bhide R, Cho Y, Chong S, Chao S, Gullo-Brown J, Guo P, Kim SH, Lee FY, Leftheris K, Miller A, Mitt T, Patel M, Penhallow BA, Ricca C, Rose WC, Schmidt R, Slusarchyk WA, Vite G, Manne V. Hunt JT, et al. J Med Chem. 2000 Oct 5;43(20):3587-95. doi: 10.1021/jm000248z. J Med Chem. 2000. PMID: 11020273
Design, synthesis, and structure-activity relationships of tetrahydroquinoline-based farnesyltransferase inhibitors.
Lombardo LJ, Camuso A, Clark J, Fager K, Gullo-Brown J, Hunt JT, Inigo I, Kan D, Koplowitz B, Lee F, McGlinchey K, Qian L, Ricca C, Rovnyak G, Traeger S, Tokarski J, Williams DK, Wu LI, Zhao Y, Manne V, Bhide RS. Lombardo LJ, et al. Among authors: bhide rs. Bioorg Med Chem Lett. 2005 Apr 1;15(7):1895-9. doi: 10.1016/j.bmcl.2005.02.004. Bioorg Med Chem Lett. 2005. PMID: 15780629
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: bhide rs. 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. J Med Chem. 2006 Apr 6;49(7):2143-6. doi: 10.1021/jm051106d. J Med Chem. 2006. PMID: 16570908
26 results