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Page 1
Discovery of BMS-986202: A Clinical Tyk2 Inhibitor that Binds to Tyk2 JH2.
Liu C, Lin J, Langevine C, Smith D, Li J, Tokarski JS, Khan J, Ruzanov M, Strnad J, Zupa-Fernandez A, Cheng L, Gillooly KM, Shuster D, Zhang Y, Thankappan A, McIntyre KW, Chaudhry C, Elzinga PA, Chiney M, Chimalakonda A, Lombardo LJ, Macor JE, Carter PH, Burke JR, Weinstein DS. Liu C, et al. Among authors: lombardo lj. J Med Chem. 2021 Jan 14;64(1):677-694. doi: 10.1021/acs.jmedchem.0c01698. Epub 2020 Dec 28. J Med Chem. 2021. PMID: 33370104
Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays.
Lombardo LJ, Lee FY, Chen P, Norris D, Barrish JC, Behnia K, Castaneda S, Cornelius LA, Das J, Doweyko AM, Fairchild C, Hunt JT, Inigo I, Johnston K, Kamath A, Kan D, Klei H, Marathe P, Pang S, Peterson R, Pitt S, Schieven GL, Schmidt RJ, Tokarski J, Wen ML, Wityak J, Borzilleri RM. Lombardo LJ, et al. J Med Chem. 2004 Dec 30;47(27):6658-61. doi: 10.1021/jm049486a. J Med Chem. 2004. PMID: 15615512
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. 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: lombardo lj. 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: lombardo lj. J Med Chem. 2006 Apr 6;49(7):2143-6. doi: 10.1021/jm051106d. J Med Chem. 2006. PMID: 16570908
Synthesis and SAR of pyrrolotriazine-4-one based Eg5 inhibitors.
Kim KS, Lu S, Cornelius LA, Lombardo LJ, Borzilleri RM, Schroeder GM, Sheng C, Rovnyak G, Crews D, Schmidt RJ, Williams DK, Bhide RS, Traeger SC, McDonnell PA, Mueller L, Sheriff S, Newitt JA, Pudzianowski AT, Yang Z, Wild R, Lee FY, Batorsky R, Ryder JS, Ortega-Nanos M, Shen H, Gottardis M, Roussell DL. Kim KS, et al. Among authors: lombardo lj. Bioorg Med Chem Lett. 2006 Aug 1;16(15):3937-42. doi: 10.1016/j.bmcl.2006.05.037. Epub 2006 May 30. Bioorg Med Chem Lett. 2006. PMID: 16730979
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. Among authors: lombardo lj. J Med Chem. 2006 Jun 29;49(13):3766-9. doi: 10.1021/jm060347y. J Med Chem. 2006. PMID: 16789733
Second generation tetrahydroquinoline-based protein farnesyltransferase inhibitors as antimalarials.
Bendale P, Olepu S, Suryadevara PK, Bulbule V, Rivas K, Nallan L, Smart B, Yokoyama K, Ankala S, Pendyala PR, Floyd D, Lombardo LJ, Williams DK, Buckner FS, Chakrabarti D, Verlinde CL, Van Voorhis WC, Gelb MH. Bendale P, et al. Among authors: lombardo lj. J Med Chem. 2007 Sep 20;50(19):4585-605. doi: 10.1021/jm0703340. Epub 2007 Aug 28. J Med Chem. 2007. PMID: 17722901 Free PMC article.
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: lombardo lj. 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
64 results