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Cyclic hydroxyamidines as amide isosteres: discovery of oxadiazolines and oxadiazines as potent and highly efficacious γ-secretase modulators in vivo.
Sun ZY, Asberom T, Bara T, Bennett C, Burnett D, Chu I, Clader J, Cohen-Williams M, Cole D, Czarniecki M, Durkin J, Gallo G, Greenlee W, Josien H, Huang X, Hyde L, Jones N, Kazakevich I, Li H, Liu X, Lee J, Maccoss M, Mandal MB, McCracken T, Nomeir A, Mazzola R, Palani A, Parker EM, Pissarnitski DA, Qin J, Song L, Terracina G, Vicarel M, Voigt J, Xu R, Zhang L, Zhang Q, Zhao Z, Zhu X, Zhu Z. Sun ZY, et al. Among authors: li h. J Med Chem. 2012 Jan 12;55(1):489-502. doi: 10.1021/jm201407j. Epub 2011 Dec 8. J Med Chem. 2012. PMID: 22098494
Design and synthesis of tricyclic sulfones as gamma-secretase inhibitors with greatly reduced Notch toxicity.
Xu R, Cole D, Asberom T, Bara T, Bennett C, Burnett DA, Clader J, Domalski M, Greenlee W, Hyde L, Josien H, Li H, McBriar M, McKittrick B, McPhail AT, Pissarnitski D, Qiang L, Rajagopalan M, Sasikumar T, Su J, Tang H, Wu WL, Zhang L, Zhao Z. Xu R, et al. Among authors: li h. Bioorg Med Chem Lett. 2010 Apr 15;20(8):2591-6. doi: 10.1016/j.bmcl.2010.02.080. Epub 2010 Feb 23. Bioorg Med Chem Lett. 2010. PMID: 20236824
The discovery of fused oxadiazepines as gamma secretase modulators for treatment of Alzheimer's disease.
Li H, Qin J, Dhondi P, Zhou W, Vicarel M, Bara T, Cole D, Josien H, Pissarnitski D, Zhu Z, Palani A, Aslanian R, Clader J, Czarniecki M, Greenlee W, Cohen-Williams M, Hyde L, Song L, Zhang L, Chu I, Huang X. Li H, et al. Bioorg Med Chem Lett. 2013 Jan 15;23(2):466-71. doi: 10.1016/j.bmcl.2012.11.055. Epub 2012 Nov 29. Bioorg Med Chem Lett. 2013. PMID: 23253441
Synthesis and SAR Studies of Fused Oxadiazines as γ-Secretase Modulators for Treatment of Alzheimer's Disease.
Huang X, Zhou W, Liu X, Li H, Sun G, Mandal M, Vicarel M, Zhu X, Bennett C, McCraken T, Pissarnitski D, Zhao Z, Cole D, Gallo G, Zhu Z, Palani A, Aslanian R, Clader J, Czarniecki M, Greenlee W, Burnett D, Cohen-Williams M, Hyde L, Song L, Zhang L, Chu I, Buevich A. Huang X, et al. Among authors: li h. ACS Med Chem Lett. 2012 Sep 4;3(11):931-5. doi: 10.1021/ml300209g. eCollection 2012 Nov 8. ACS Med Chem Lett. 2012. PMID: 24900409 Free PMC article.
Discovery of a Novel, Potent Spirocyclic Series of γ-Secretase Inhibitors.
Zhao Z, Pissarnitski DA, Josien HB, Wu WL, Xu R, Li H, Clader JW, Burnett DA, Terracina G, Hyde L, Lee J, Song L, Zhang L, Parker EM. Zhao Z, et al. Among authors: li h. J Med Chem. 2015 Nov 25;58(22):8806-17. doi: 10.1021/acs.jmedchem.5b00774. Epub 2015 Nov 6. J Med Chem. 2015. PMID: 26496070
Substituted 4-morpholine N-arylsulfonamides as γ-secretase inhibitors.
Zhao Z, Pissarnitski DA, Josien HB, Bara TA, Clader JW, Li H, McBriar MD, Rajagopalan M, Xu R, Terracina G, Hyde L, Song L, Zhang L, Parker EM, Osterman R, Buevich AV. Zhao Z, et al. Among authors: li h. Eur J Med Chem. 2016 Nov 29;124:36-48. doi: 10.1016/j.ejmech.2016.08.024. Epub 2016 Aug 13. Eur J Med Chem. 2016. PMID: 27560281
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