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Design and synthesis of highly potent benzodiazepine gamma-secretase inhibitors: preparation of (2S,3R)-3-(3,4-difluorophenyl)-2-(4-fluorophenyl)-4- hydroxy-N-((3S)-1-methyl-2-oxo-5- phenyl-2,3-dihydro-1H-benzo[e][1,4]-diazepin-3-yl)butyramide by use of an asymmetric Ireland-Claisen rearrangement.
Churcher I, Williams S, Kerrad S, Harrison T, Castro JL, Shearman MS, Lewis HD, Clarke EE, Wrigley JD, Beher D, Tang YS, Liu W. Churcher I, et al. Among authors: castro jl. J Med Chem. 2003 Jun 5;46(12):2275-8. doi: 10.1021/jm034058a. J Med Chem. 2003. PMID: 12773031
Aryl sulfones: a new class of gamma-secretase inhibitors.
Teall M, Oakley P, Harrison T, Shaw D, Kay E, Elliott J, Gerhard U, Castro JL, Shearman M, Ball RG, Tsou NN. Teall M, et al. Among authors: castro jl. Bioorg Med Chem Lett. 2005 May 16;15(10):2685-8. doi: 10.1016/j.bmcl.2004.12.017. Bioorg Med Chem Lett. 2005. PMID: 15863342
Cyclic sulfamide gamma-secretase inhibitors.
Sparey T, Beher D, Best J, Biba M, Castro JL, Clarke E, Hannam J, Harrison T, Lewis H, Madin A, Shearman M, Sohal B, Tsou N, Welch C, Wrigley J. Sparey T, et al. Among authors: castro jl. Bioorg Med Chem Lett. 2005 Oct 1;15(19):4212-6. doi: 10.1016/j.bmcl.2005.06.084. Bioorg Med Chem Lett. 2005. PMID: 16054361
4-substituted cyclohexyl sulfones as potent, orally active gamma-secretase inhibitors.
Churcher I, Beher D, Best JD, Castro JL, Clarke EE, Gentry A, Harrison T, Hitzel L, Kay E, Kerrad S, Lewis HD, Morentin-Gutierrez P, Mortishire-Smith R, Oakley PJ, Reilly M, Shaw DE, Shearman MS, Teall MR, Williams S, Wrigley JD. Churcher I, et al. Among authors: castro jl. Bioorg Med Chem Lett. 2006 Jan 15;16(2):280-4. doi: 10.1016/j.bmcl.2005.10.009. Epub 2005 Nov 3. Bioorg Med Chem Lett. 2006. PMID: 16275079
gamma-Secretase: characterization and implication for Alzheimer disease therapy.
Xu M, Lai MT, Huang Q, DiMuzio-Mower J, Castro JL, Harrison T, Nadin A, Neduvelil JG, Shearman MS, Shafer JA, Gardell SJ, Li YM. Xu M, et al. Among authors: castro jl. Neurobiol Aging. 2002 Nov-Dec;23(6):1023-30. doi: 10.1016/s0197-4580(02)00126-4. Neurobiol Aging. 2002. PMID: 12470798
204 results