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Page 1
The Discovery and Hit-to-Lead Optimization of Tricyclic Sulfonamides as Potent and Efficacious Potentiators of Glycine Receptors.
Bregman H, Simard JR, Andrews KL, Ayube S, Chen H, Gunaydin H, Guzman-Perez A, Hu J, Huang L, Huang X, Krolikowski PH, Lehto SG, Lewis RT, Michelsen K, Pegman P, Plant MH, Shaffer PL, Teffera Y, Yi S, Zhang M, Gingras J, DiMauro EF. Bregman H, et al. Among authors: lewis rt. J Med Chem. 2017 Feb 9;60(3):1105-1125. doi: 10.1021/acs.jmedchem.6b01496. Epub 2016 Dec 21. J Med Chem. 2017. PMID: 28001399
The discovery and optimization of a novel class of potent, selective, and orally bioavailable anaplastic lymphoma kinase (ALK) inhibitors with potential utility for the treatment of cancer.
Lewis RT, Bode CM, Choquette DM, Potashman M, Romero K, Stellwagen JC, Teffera Y, Moore E, Whittington DA, Chen H, Epstein LF, Emkey R, Andrews PS, Yu VL, Saffran DC, Xu M, Drew A, Merkel P, Szilvassy S, Brake RL. Lewis RT, et al. J Med Chem. 2012 Jul 26;55(14):6523-40. doi: 10.1021/jm3005866. Epub 2012 Jul 10. J Med Chem. 2012. PMID: 22734674
Discovery of potent and selective 8-fluorotriazolopyridine c-Met inhibitors.
Peterson EA, Teffera Y, Albrecht BK, Bauer D, Bellon SF, Boezio A, Boezio C, Broome MA, Choquette D, Copeland KW, Dussault I, Lewis R, Lin MH, Lohman J, Liu J, Potashman M, Rex K, Shimanovich R, Whittington DA, Vaida KR, Harmange JC. Peterson EA, et al. J Med Chem. 2015 Mar 12;58(5):2417-30. doi: 10.1021/jm501913a. Epub 2015 Mar 3. J Med Chem. 2015. PMID: 25699405
Discovery of (R)-6-(1-(8-Fluoro-6-(1-methyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-a]pyridin-3-yl)ethyl)-3-(2-methoxyethoxy)-1,6-naphthyridin-5(6H)-one (AMG 337), a Potent and Selective Inhibitor of MET with High Unbound Target Coverage and Robust In Vivo Antitumor Activity.
Boezio AA, Copeland KW, Rex K, K Albrecht B, Bauer D, Bellon SF, Boezio C, Broome MA, Choquette D, Coxon A, Dussault I, Hirai S, Lewis R, Lin MH, Lohman J, Liu J, Peterson EA, Potashman M, Shimanovich R, Teffera Y, Whittington DA, Vaida KR, Harmange JC. Boezio AA, et al. J Med Chem. 2016 Mar 24;59(6):2328-42. doi: 10.1021/acs.jmedchem.5b01716. Epub 2016 Feb 11. J Med Chem. 2016. PMID: 26812066
Discovery and optimization of potent and selective imidazopyridine and imidazopyridazine mTOR inhibitors.
Peterson EA, Boezio AA, Andrews PS, Boezio CM, Bush TL, Cheng AC, Choquette D, Coats JR, Colletti AE, Copeland KW, DuPont M, Graceffa R, Grubinska B, Kim JL, Lewis RT, Liu J, Mullady EL, Potashman MH, Romero K, Shaffer PL, Stanton MK, Stellwagen JC, Teffera Y, Yi S, Cai T, La DS. Peterson EA, et al. Among authors: lewis rt. Bioorg Med Chem Lett. 2012 Aug 1;22(15):4967-74. doi: 10.1016/j.bmcl.2012.06.033. Epub 2012 Jun 16. Bioorg Med Chem Lett. 2012. PMID: 22765895
Purinylpyridinylamino-based DFG-in/αC-helix-out B-Raf inhibitors: Applying mutant versus wild-type B-Raf selectivity indices for compound profiling.
Liu L, Lee MR, Kim JL, Whittington DA, Bregman H, Hua Z, Lewis RT, Martin MW, Nishimura N, Potashman M, Yang K, Yi S, Vaida KR, Epstein LF, Babij C, Fernando M, Carnahan J, Norman MH. Liu L, et al. Among authors: lewis rt. Bioorg Med Chem. 2016 May 15;24(10):2215-34. doi: 10.1016/j.bmc.2016.03.055. Epub 2016 Apr 13. Bioorg Med Chem. 2016. PMID: 27085672
Corrigendum to "Purinylpyridinylamino-based DFG-in/αC-helix-out B-Raf inhibitors: Applying mutant versus wild-type B-Raf selectivity indices for compound profiling" [Bioorg. Med. Chem. 24 (2016) 2215-2234].
Liu L, Lee MR, Kim JL, Whittington DA, Bregman H, Hua Z, Lewis RT, Martin MW, Nishimura N, Potashman M, Yang K, Yi S, Vaida KR, Epstein LF, Babij C, Fernando M, Carnahan J, Norman MH. Liu L, et al. Among authors: lewis rt. Bioorg Med Chem. 2016 Jul 1;24(13):3093. doi: 10.1016/j.bmc.2016.05.014. Epub 2016 May 24. Bioorg Med Chem. 2016. PMID: 27234892 No abstract available.
Correction to Discovery of Potent and Selective 8-Fluorotriazolopyridine c-Met Inhibitors.
Peterson EA, Teffera Y, Albrecht BK, Bauer D, Bellon SF, Boezio A, Boezio C, Broome MA, Choquette D, Copeland KW, Dussault I, Lewis R, Lin MH, Lohman J, Liu J, Potashman M, Rex K, Shimanovich R, Whittington DA, Vaida KR, Harmange JC. Peterson EA, et al. J Med Chem. 2015 May 14;58(9):4087. doi: 10.1021/acs.jmedchem.5b00591. Epub 2015 Apr 22. J Med Chem. 2015. PMID: 25901648 No abstract available.
82 results