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Page 1
Acylguanidines as small-molecule beta-secretase inhibitors.
Cole DC, Manas ES, Stock JR, Condon JS, Jennings LD, Aulabaugh A, Chopra R, Cowling R, Ellingboe JW, Fan KY, Harrison BL, Hu Y, Jacobsen S, Jin G, Lin L, Lovering FE, Malamas MS, Stahl ML, Strand J, Sukhdeo MN, Svenson K, Turner MJ, Wagner E, Wu J, Zhou P, Bard J. Cole DC, et al. Among authors: fan ky. J Med Chem. 2006 Oct 19;49(21):6158-61. doi: 10.1021/jm0607451. J Med Chem. 2006. PMID: 17034121
Acylguanidine inhibitors of beta-secretase: optimization of the pyrrole ring substituents extending into the S1' substrate binding pocket.
Jennings LD, Cole DC, Stock JR, Sukhdeo MN, Ellingboe JW, Cowling R, Jin G, Manas ES, Fan KY, Malamas MS, Harrison BL, Jacobsen S, Chopra R, Lohse PA, Moore WJ, O'Donnell MM, Hu Y, Robichaud AJ, Turner MJ, Wagner E, Bard J. Jennings LD, et al. Bioorg Med Chem Lett. 2008 Jan 15;18(2):767-71. doi: 10.1016/j.bmcl.2007.11.043. Epub 2007 Nov 17. Bioorg Med Chem Lett. 2008. PMID: 18068983
Acylguanidine inhibitors of beta-secretase: optimization of the pyrrole ring substituents extending into the S1 and S3 substrate binding pockets.
Cole DC, Stock JR, Chopra R, Cowling R, Ellingboe JW, Fan KY, Harrison BL, Hu Y, Jacobsen S, Jennings LD, Jin G, Lohse PA, Malamas MS, Manas ES, Moore WJ, O'Donnell MM, Olland AM, Robichaud AJ, Svenson K, Wu J, Wagner E, Bard J. Cole DC, et al. Among authors: fan ky. Bioorg Med Chem Lett. 2008 Feb 1;18(3):1063-6. doi: 10.1016/j.bmcl.2007.12.010. Epub 2007 Dec 10. Bioorg Med Chem Lett. 2008. PMID: 18162398
Discovery and initial optimization of 5,5'-disubstituted aminohydantoins as potent beta-secretase (BACE1) inhibitors.
Nowak P, Cole DC, Aulabaugh A, Bard J, Chopra R, Cowling R, Fan KY, Hu B, Jacobsen S, Jani M, Jin G, Lo MC, Malamas MS, Manas ES, Narasimhan R, Reinhart P, Robichaud AJ, Stock JR, Subrath J, Svenson K, Turner J, Wagner E, Zhou P, Ellingboe JW. Nowak P, et al. Among authors: fan ky. Bioorg Med Chem Lett. 2010 Jan 15;20(2):632-5. doi: 10.1016/j.bmcl.2009.11.052. Epub 2009 Nov 20. Bioorg Med Chem Lett. 2010. PMID: 19959359
Synthesis and SAR of bis-statine based peptides as BACE 1 inhibitors.
Hu B, Fan KY, Bridges K, Chopra R, Lovering F, Cole D, Zhou P, Ellingboe J, Jin G, Cowling R, Bard J. Hu B, et al. Among authors: fan ky. Bioorg Med Chem Lett. 2004 Jul 5;14(13):3457-60. doi: 10.1016/j.bmcl.2004.04.068. Bioorg Med Chem Lett. 2004. PMID: 15177452
Highly potent, selective, and orally active phosphodiesterase 10A inhibitors.
Malamas MS, Ni Y, Erdei J, Stange H, Schindler R, Lankau HJ, Grunwald C, Fan KY, Parris K, Langen B, Egerland U, Hage T, Marquis KL, Grauer S, Brennan J, Navarra R, Graf R, Harrison BL, Robichaud A, Kronbach T, Pangalos MN, Hoefgen N, Brandon NJ. Malamas MS, et al. Among authors: fan ky. J Med Chem. 2011 Nov 10;54(21):7621-38. doi: 10.1021/jm2009138. Epub 2011 Oct 11. J Med Chem. 2011. PMID: 21988093
Novel triazines as potent and selective phosphodiesterase 10A inhibitors.
Malamas MS, Stange H, Schindler R, Lankau HJ, Grunwald C, Langen B, Egerland U, Hage T, Ni Y, Erdei J, Fan KY, Parris K, Marquis KL, Grauer S, Brennan J, Navarra R, Graf R, Harrison BL, Robichaud A, Kronbach T, Pangalos MN, Brandon NJ, Hoefgen N. Malamas MS, et al. Among authors: fan ky. Bioorg Med Chem Lett. 2012 Sep 15;22(18):5876-84. doi: 10.1016/j.bmcl.2012.07.076. Epub 2012 Jul 31. Bioorg Med Chem Lett. 2012. PMID: 22902656
Discovery of begacestat, a Notch-1-sparing gamma-secretase inhibitor for the treatment of Alzheimer's disease.
Mayer SC, Kreft AF, Harrison B, Abou-Gharbia M, Antane M, Aschmies S, Atchison K, Chlenov M, Cole DC, Comery T, Diamantidis G, Ellingboe J, Fan K, Galante R, Gonzales C, Ho DM, Hoke ME, Hu Y, Huryn D, Jain U, Jin M, Kremer K, Kubrak D, Lin M, Lu P, Magolda R, Martone R, Moore W, Oganesian A, Pangalos MN, Porte A, Reinhart P, Resnick L, Riddell DR, Sonnenberg-Reines J, Stock JR, Sun SC, Wagner E, Wang T, Woller K, Xu Z, Zaleska MM, Zeldis J, Zhang M, Zhou H, Jacobsen JS. Mayer SC, et al. Among authors: fan k. J Med Chem. 2008 Dec 11;51(23):7348-51. doi: 10.1021/jm801252w. J Med Chem. 2008. PMID: 19012391
2,613 results