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A new series of potent benzodiazepine gamma-secretase inhibitors.
Churcher I, Ashton K, Butcher JW, Clarke EE, Harrison T, Lewis HD, Owens AP, Teall MR, Williams S, Wrigley JD. Churcher I, et al. Bioorg Med Chem Lett. 2003 Jan 20;13(2):179-83. doi: 10.1016/s0960-894x(02)00909-5. Bioorg Med Chem Lett. 2003. PMID: 12482419
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. 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
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: lewis h. 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
The novel gamma secretase inhibitor N-[cis-4-[(4-chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexyl]-1,1,1-trifluoromethanesulfonamide (MRK-560) reduces amyloid plaque deposition without evidence of notch-related pathology in the Tg2576 mouse.
Best JD, Smith DW, Reilly MA, O'Donnell R, Lewis HD, Ellis S, Wilkie N, Rosahl TW, Laroque PA, Boussiquet-Leroux C, Churcher I, Atack JR, Harrison T, Shearman MS. Best JD, et al. J Pharmacol Exp Ther. 2007 Feb;320(2):552-8. doi: 10.1124/jpet.106.114330. Epub 2006 Nov 10. J Pharmacol Exp Ther. 2007. PMID: 17099072
1,171 results