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Page 1
Discovery of novel hydroxamates as highly potent tumor necrosis factor-alpha converting enzyme inhibitors. Part II: optimization of the S3' pocket.
Mazzola RD Jr, Zhu Z, Sinning L, McKittrick B, Lavey B, Spitler J, Kozlowski J, Neng-Yang S, Zhou G, Guo Z, Orth P, Madison V, Sun J, Lundell D, Niu X. Mazzola RD Jr, et al. Among authors: mckittrick b. Bioorg Med Chem Lett. 2008 Nov 1;18(21):5809-14. doi: 10.1016/j.bmcl.2008.09.045. Epub 2008 Sep 13. Bioorg Med Chem Lett. 2008. PMID: 18835710
The discovery of novel tartrate-based TNF-alpha converting enzyme (TACE) inhibitors.
Rosner KE, Guo Z, Orth P, Shipps GW Jr, Belanger DB, Chan TY, Curran PJ, Dai C, Deng Y, Girijavallabhan VM, Hong L, Lavey BJ, Lee JF, Li D, Liu Z, Popovici-Muller J, Ting PC, Vaccaro H, Wang L, Wang T, Yu W, Zhou G, Niu X, Sun J, Kozlowski JA, Lundell DJ, Madison V, McKittrick B, Piwinski JJ, Shih NY, Arshad Siddiqui M, Strickland CO. Rosner KE, et al. Among authors: mckittrick b. Bioorg Med Chem Lett. 2010 Feb 1;20(3):1189-93. doi: 10.1016/j.bmcl.2009.12.004. Epub 2009 Dec 5. Bioorg Med Chem Lett. 2010. PMID: 20022498
Structure and activity relationships of tartrate-based TACE inhibitors.
Li D, Popovici-Muller J, Belanger DB, Caldwell J, Dai C, David M, Girijavallabhan VM, Lavey BJ, Lee JF, Liu Z, Mazzola R, Rizvi R, Rosner KE, Shankar B, Spitler J, Ting PC, Vaccaro H, Yu W, Zhou G, Zhu Z, Niu X, Sun J, Guo Z, Orth P, Chen S, Kozlowski JA, Lundell DJ, Madison V, McKittrick B, Piwinski JJ, Shih NY, Shipps GW Jr, Siddiqui MA, Strickland CO. Li D, et al. Among authors: mckittrick b. Bioorg Med Chem Lett. 2010 Aug 15;20(16):4812-5. doi: 10.1016/j.bmcl.2010.06.104. Epub 2010 Jun 25. Bioorg Med Chem Lett. 2010. PMID: 20638281
Discovery of potent iminoheterocycle BACE1 inhibitors.
Caldwell JP, Mazzola RD, Durkin J, Chen J, Chen X, Favreau L, Kennedy M, Kuvelkar R, Lee J, McHugh N, McKittrick B, Orth P, Stamford A, Strickland C, Voigt J, Wang L, Zhang L, Zhang Q, Zhu Z. Caldwell JP, et al. Among authors: mckittrick b. Bioorg Med Chem Lett. 2014 Dec 1;24(23):5455-9. doi: 10.1016/j.bmcl.2014.10.006. Epub 2014 Oct 23. Bioorg Med Chem Lett. 2014. PMID: 25455483
Discovery of cyclic acylguanidines as highly potent and selective beta-site amyloid cleaving enzyme (BACE) inhibitors: Part I--inhibitor design and validation.
Zhu Z, Sun ZY, Ye Y, Voigt J, Strickland C, Smith EM, Cumming J, Wang L, Wong J, Wang YS, Wyss DF, Chen X, Kuvelkar R, Kennedy ME, Favreau L, Parker E, McKittrick BA, Stamford A, Czarniecki M, Greenlee W, Hunter JC. Zhu Z, et al. J Med Chem. 2010 Feb 11;53(3):951-65. doi: 10.1021/jm901408p. J Med Chem. 2010. PMID: 20043696
Application of fragment-based NMR screening, X-ray crystallography, structure-based design, and focused chemical library design to identify novel microM leads for the development of nM BACE-1 (beta-site APP cleaving enzyme 1) inhibitors.
Wang YS, Strickland C, Voigt JH, Kennedy ME, Beyer BM, Senior MM, Smith EM, Nechuta TL, Madison VS, Czarniecki M, McKittrick BA, Stamford AW, Parker EM, Hunter JC, Greenlee WJ, Wyss DF. Wang YS, et al. J Med Chem. 2010 Feb 11;53(3):942-50. doi: 10.1021/jm901472u. J Med Chem. 2010. PMID: 20043700
Design and validation of bicyclic iminopyrimidinones as beta amyloid cleaving enzyme-1 (BACE1) inhibitors: conformational constraint to favor a bioactive conformation.
Mandal M, Zhu Z, Cumming JN, Liu X, Strickland C, Mazzola RD, Caldwell JP, Leach P, Grzelak M, Hyde L, Zhang Q, Terracina G, Zhang L, Chen X, Kuvelkar R, Kennedy ME, Favreau L, Cox K, Orth P, Buevich A, Voigt J, Wang H, Kazakevich I, McKittrick BA, Greenlee W, Parker EM, Stamford AW. Mandal M, et al. Among authors: mckittrick ba. J Med Chem. 2012 Nov 8;55(21):9331-45. doi: 10.1021/jm301039c. Epub 2012 Oct 1. J Med Chem. 2012. PMID: 22989333
Pyrazolo[1,5-a]pyrimidines as orally available inhibitors of cyclin-dependent kinase 2.
Paruch K, Dwyer MP, Alvarez C, Brown C, Chan TY, Doll RJ, Keertikar K, Knutson C, McKittrick B, Rivera J, Rossman R, Tucker G, Fischmann TO, Hruza A, Madison V, Nomeir AA, Wang Y, Lees E, Parry D, Sgambellone N, Seghezzi W, Schultz L, Shanahan F, Wiswell D, Xu X, Zhou Q, James RA, Paradkar VM, Park H, Rokosz LR, Stauffer TM, Guzi TJ. Paruch K, et al. Among authors: mckittrick b. Bioorg Med Chem Lett. 2007 Nov 15;17(22):6220-3. doi: 10.1016/j.bmcl.2007.09.017. Epub 2007 Sep 8. Bioorg Med Chem Lett. 2007. PMID: 17904841
Design and discovery of 1,3-benzodiazepines as novel dopamine antagonists.
Zhu Z, Sun ZY, Ye Y, McKittrick B, Greenlee W, Czarniecki M, Fawzi A, Zhang H, Lachowicz JE. Zhu Z, et al. Among authors: mckittrick b. Bioorg Med Chem Lett. 2009 Sep 1;19(17):5218-21. doi: 10.1016/j.bmcl.2009.07.012. Epub 2009 Jul 9. Bioorg Med Chem Lett. 2009. PMID: 19643610
42 results