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Page 1
High-resolution crystal structures of factor XIa coagulation factor in complex with nonbasic high-affinity synthetic inhibitors.
Fradera X, Kazemier B, Carswell E, Cooke A, Oubrie A, Hamilton W, Dempster M, Krapp S, Nagel S, Jestel A. Fradera X, et al. Among authors: hamilton w. Acta Crystallogr Sect F Struct Biol Cryst Commun. 2012 Apr 1;68(Pt 4):404-8. doi: 10.1107/S1744309112009037. Epub 2012 Mar 27. Acta Crystallogr Sect F Struct Biol Cryst Commun. 2012. PMID: 22505407 Free PMC article.
6-Phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile as cathepsin S inhibitors.
Cai J, Baugh M, Black D, Long C, Jonathan Bennett D, Dempster M, Fradera X, Gillespie J, Andrews F, Boucharens S, Bruin J, Cameron KS, Cumming I, Hamilton W, Jones PS, Kaptein A, Kinghorn E, Maidment M, Martin I, Mitchell A, Rankovic Z, Robinson J, Scullion P, Uitdehaag JC, Vink P, Westwood P, van Zeeland M, van Berkom L, Bastiani M, Meulemans T. Cai J, et al. Among authors: hamilton w. Bioorg Med Chem Lett. 2010 Aug 1;20(15):4350-4. doi: 10.1016/j.bmcl.2010.06.072. Epub 2010 Jun 17. Bioorg Med Chem Lett. 2010. PMID: 20598883
4-(3-Trifluoromethylphenyl)-pyrimidine-2-carbonitrile as cathepsin S inhibitors: N3, not N1 is critically important.
Cai J, Fradera X, van Zeeland M, Dempster M, Cameron KS, Bennett DJ, Robinson J, Popplestone L, Baugh M, Westwood P, Bruin J, Hamilton W, Kinghorn E, Long C, Uitdehaag JC. Cai J, et al. Among authors: hamilton w. Bioorg Med Chem Lett. 2010 Aug 1;20(15):4507-10. doi: 10.1016/j.bmcl.2010.06.043. Epub 2010 Jun 10. Bioorg Med Chem Lett. 2010. PMID: 20580231
Design and optimization of a series of novel 2-cyano-pyrimidines as cathepsin K inhibitors.
Rankovic Z, Cai J, Kerr J, Fradera X, Robinson J, Mistry A, Hamilton E, McGarry G, Andrews F, Caulfield W, Cumming I, Dempster M, Waller J, Scullion P, Martin I, Mitchell A, Long C, Baugh M, Westwood P, Kinghorn E, Bruin J, Hamilton W, Uitdehaag J, van Zeeland M, Potin D, Saniere L, Fouquet A, Chevallier F, Deronzier H, Dorleans C, Nicolai E. Rankovic Z, et al. Among authors: hamilton e, hamilton w. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1524-7. doi: 10.1016/j.bmcl.2010.01.100. Epub 2010 Jan 25. Bioorg Med Chem Lett. 2010. PMID: 20149657
1H-imidazo[4,5-c]pyridine-4-carbonitrile as cathepsin S inhibitors: separation of desired cellular activity from undesired tissue accumulation through optimization of basic nitrogen pka.
Arbuckle W, Baugh M, Belshaw S, Bennett DJ, Bruin J, Cai J, Cameron KS, Claxton C, Dempster M, Everett K, Fradera X, Hamilton W, Jones PS, Kinghorn E, Long C, Martin I, Robinson J, Westwood P. Arbuckle W, et al. Among authors: hamilton w. Bioorg Med Chem Lett. 2011 Feb 1;21(3):932-5. doi: 10.1016/j.bmcl.2010.12.065. Epub 2010 Dec 19. Bioorg Med Chem Lett. 2011. PMID: 21227690
2-Phenyl-9H-purine-6-carbonitrile derivatives as selective cathepsin S inhibitors.
Cai J, Bennett DJ, Rankovic Z, Dempster M, Fradera X, Gillespie J, Cumming I, Finlay W, Baugh M, Boucharens S, Bruin J, Cameron KS, Hamilton W, Kerr J, Kinghorn E, McGarry G, Robinson J, Scullion P, Uitdehaag JC, van Zeeland M, Potin D, Saniere L, Fouquet A, Chevallier F, Deronzier H, Dorleans C, Nicolai E. Cai J, et al. Among authors: hamilton w. Bioorg Med Chem Lett. 2010 Aug 1;20(15):4447-50. doi: 10.1016/j.bmcl.2010.06.049. Epub 2010 Jun 15. Bioorg Med Chem Lett. 2010. PMID: 20594841
Trifluoromethylphenyl as P2 for ketoamide-based cathepsin S inhibitors.
Cai J, Robinson J, Belshaw S, Everett K, Fradera X, van Zeeland M, van Berkom L, van Rijnsbergen P, Popplestone L, Baugh M, Dempster M, Bruin J, Hamilton W, Kinghorn E, Westwood P, Kerr J, Rankovic Z, Arbuckle W, Bennett DJ, Jones PS, Long C, Martin I, Uitdehaag JC, Meulemans T. Cai J, et al. Among authors: hamilton w. Bioorg Med Chem Lett. 2010 Dec 1;20(23):6890-4. doi: 10.1016/j.bmcl.2010.10.012. Epub 2010 Oct 26. Bioorg Med Chem Lett. 2010. PMID: 21030256
Therapeutic dosing of an orally active, selective cathepsin S inhibitor suppresses disease in models of autoimmunity.
Baugh M, Black D, Westwood P, Kinghorn E, McGregor K, Bruin J, Hamilton W, Dempster M, Claxton C, Cai J, Bennett J, Long C, McKinnon H, Vink P, den Hoed L, Gorecka M, Vora K, Grant E, Percival MD, Boots AM, van Lierop MJ. Baugh M, et al. Among authors: hamilton w. J Autoimmun. 2011 May;36(3-4):201-9. doi: 10.1016/j.jaut.2011.01.003. Epub 2011 Mar 24. J Autoimmun. 2011. PMID: 21439785
Discovery and SAR of org 24598-a selective glycine uptake inhibitor.
Brown A, Carlyle I, Clark J, Hamilton W, Gibson S, McGarry G, McEachen S, Rae D, Thorn S, Walker G. Brown A, et al. Among authors: hamilton w. Bioorg Med Chem Lett. 2001 Aug 6;11(15):2007-9. doi: 10.1016/s0960-894x(01)00355-9. Bioorg Med Chem Lett. 2001. PMID: 11454468
1,430 results