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Page 1
Discovery of novel aspartyl ketone dipeptides as potent and selective caspase-3 inhibitors.
Han Y, Giroux A, Grimm EL, Aspiotis R, Francoeur S, Bayly CI, Mckay DJ, Roy S, Xanthoudakis S, Vaillancourt JP, Rasper DM, Tam J, Tawa P, Thornberry NA, Paterson EP, Garcia-Calvo M, Becker JW, Rotonda J, Nicholson DW, Zamboni RJ. Han Y, et al. Among authors: mckay dj. Bioorg Med Chem Lett. 2004 Feb 9;14(3):805-8. doi: 10.1016/j.bmcl.2003.10.064. Bioorg Med Chem Lett. 2004. PMID: 14741294
Reducing the peptidyl features of caspase-3 inhibitors: a structural analysis.
Becker JW, Rotonda J, Soisson SM, Aspiotis R, Bayly C, Francoeur S, Gallant M, Garcia-Calvo M, Giroux A, Grimm E, Han Y, McKay D, Nicholson DW, Peterson E, Renaud J, Roy S, Thornberry N, Zamboni R. Becker JW, et al. J Med Chem. 2004 May 6;47(10):2466-74. doi: 10.1021/jm0305523. J Med Chem. 2004. PMID: 15115390
Identification of a new biaryl scaffold generating potent renin inhibitors.
Lacombe P, Aspiotis R, Bayly C, Chen A, Dubé D, Fortin R, Gallant M, Juteau H, Liu S, McKay D, Roy P, Wu T. Lacombe P, et al. Bioorg Med Chem Lett. 2010 Oct 1;20(19):5822-6. doi: 10.1016/j.bmcl.2010.07.127. Epub 2010 Aug 3. Bioorg Med Chem Lett. 2010. PMID: 20728350
The discovery and synthesis of potent zwitterionic inhibitors of renin.
Aspiotis R, Chen A, Cauchon E, Dubé D, Falgueyret JP, Gagné S, Gallant M, Grimm EL, Houle R, Juteau H, Lacombe P, Laliberté S, Lévesque JF, MacDonald D, McKay D, Percival MD, Roy P, Soisson SM, Wu T. Aspiotis R, et al. Bioorg Med Chem Lett. 2011 Apr 15;21(8):2430-6. doi: 10.1016/j.bmcl.2011.02.067. Epub 2011 Feb 18. Bioorg Med Chem Lett. 2011. PMID: 21429746
Nicotinyl aspartyl ketones as inhibitors of caspase-3.
Isabel E, Black WC, Bayly CI, Grimm EL, Janes MK, McKay DJ, Nicholson DW, Rasper DM, Renaud J, Roy S, Tam J, Thornberry NA, Vaillancourt JP, Xanthoudakis S, Zamboni R. Isabel E, et al. Among authors: mckay dj. Bioorg Med Chem Lett. 2003 Jul 7;13(13):2137-40. doi: 10.1016/s0960-894x(03)00390-1. Bioorg Med Chem Lett. 2003. PMID: 12798321
Novel pyrazinone mono-amides as potent and reversible caspase-3 inhibitors.
Han Y, Giroux A, Colucci J, Bayly CI, Mckay DJ, Roy S, Xanthoudakis S, Vaillancourt J, Rasper DM, Tam J, Tawa P, Nicholson DW, Zamboni RJ. Han Y, et al. Among authors: mckay dj. Bioorg Med Chem Lett. 2005 Feb 15;15(4):1173-80. doi: 10.1016/j.bmcl.2004.12.006. Bioorg Med Chem Lett. 2005. PMID: 15686936
Lipophilic versus hydrogen-bonding effect in P3 on potency and selectivity of valine aspartyl ketones as caspase 3 inhibitors.
Mellon C, Aspiotis R, Black CW, Bayly CI, Grimm EL, Giroux A, Han Y, Isabel E, McKay DJ, Nicholson DW, Rasper DM, Roy S, Tam J, Thornberry NA, Vaillancourt JP, Xanthoudakis S, Zamboni R. Mellon C, et al. Among authors: mckay dj. Bioorg Med Chem Lett. 2005 Sep 1;15(17):3886-90. doi: 10.1016/j.bmcl.2005.05.116. Bioorg Med Chem Lett. 2005. PMID: 16023344
Trifluoroethylamines as amide isosteres in inhibitors of cathepsin K.
Black WC, Bayly CI, Davis DE, Desmarais S, Falgueyret JP, Léger S, Li CS, Massé F, McKay DJ, Palmer JT, Percival MD, Robichaud J, Tsou N, Zamboni R. Black WC, et al. Among authors: mckay dj. Bioorg Med Chem Lett. 2005 Nov 1;15(21):4741-4. doi: 10.1016/j.bmcl.2005.07.071. Bioorg Med Chem Lett. 2005. PMID: 16154747
Design and optimization of a substituted amino propanamide series of renin inhibitors for the treatment of hypertension.
Chen A, Bayly C, Bezençon O, Richard-Bildstein S, Dubé D, Dubé L, Gagné S, Gallant M, Gaudreault M, Grimm E, Houle R, Lacombe P, Laliberté S, Lévesque JF, Liu S, MacDonald D, Mackay B, Martin D, McKay D, Powell D, Remen L, Soisson S, Toulmond S. Chen A, et al. Bioorg Med Chem Lett. 2010 Apr 1;20(7):2204-9. doi: 10.1016/j.bmcl.2010.02.036. Epub 2010 Feb 18. Bioorg Med Chem Lett. 2010. PMID: 20206513
96 results