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Page 1
Structure-activity relationship (SAR) studies on substituted N-(pyridin-3-yl)-2-amino-isonicotinamides as highly potent and selective glycogen synthase kinase-3 (GSK-3) inhibitors.
Luo G, Chen L, Jacutin-Porte S, Han Y, Burton CR, Xiao H, Krause CM, Cao Y, Liu N, Kish K, Lewis HA, Macor JE, Dubowchik GM. Luo G, et al. Among authors: burton cr. Bioorg Med Chem Lett. 2023 Feb 1;81:129143. doi: 10.1016/j.bmcl.2023.129143. Epub 2023 Jan 18. Bioorg Med Chem Lett. 2023. PMID: 36669575
Identification of selective inhibitors of cyclin dependent kinase 4.
Carini DJ, Kaltenbach RF, Liu J, Benfield PA, Boylan J, Boisclair M, Brizuela L, Burton CR, Cox S, Grafstrom R, Harrison BA, Harrison K, Akamike E, Markwalder JA, Nakano Y, Seitz SP, Sharp DM, Trainor GL, Sielecki TM. Carini DJ, et al. Among authors: burton cr. Bioorg Med Chem Lett. 2001 Aug 20;11(16):2209-11. doi: 10.1016/s0960-894x(01)00416-4. Bioorg Med Chem Lett. 2001. PMID: 11514172
Synthesis and evaluation of indenopyrazoles as cyclin-dependent kinase inhibitors. 3. Structure activity relationships at C3(1,2).
Yue EW, Higley CA, DiMeo SV, Carini DJ, Nugiel DA, Benware C, Benfield PA, Burton CR, Cox S, Grafstrom RH, Sharp DM, Sisk LM, Boylan JF, Muckelbauer JK, Smallwood AM, Chen H, Chang CH, Seitz SP, Trainor GL. Yue EW, et al. Among authors: burton cr. J Med Chem. 2002 Nov 21;45(24):5233-48. doi: 10.1021/jm0201722. J Med Chem. 2002. PMID: 12431051
Synthesis and biological evaluation of 1-aryl-4,5-dihydro-1H-pyrazolo[3,4-d]pyrimidin-4-one inhibitors of cyclin-dependent kinases.
Markwalder JA, Arnone MR, Benfield PA, Boisclair M, Burton CR, Chang CH, Cox SS, Czerniak PM, Dean CL, Doleniak D, Grafstrom R, Harrison BA, Kaltenbach RF 3rd, Nugiel DA, Rossi KA, Sherk SR, Sisk LM, Stouten P, Trainor GL, Worland P, Seitz SP. Markwalder JA, et al. Among authors: burton cr. J Med Chem. 2004 Nov 18;47(24):5894-911. doi: 10.1021/jm020455u. J Med Chem. 2004. PMID: 15537345
P-glycoprotein efflux and other factors limit brain amyloid beta reduction by beta-site amyloid precursor protein-cleaving enzyme 1 inhibitors in mice.
Meredith JE Jr, Thompson LA, Toyn JH, Marcin L, Barten DM, Marcinkeviciene J, Kopcho L, Kim Y, Lin A, Guss V, Burton C, Iben L, Polson C, Cantone J, Ford M, Drexler D, Fiedler T, Lentz KA, Grace JE Jr, Kolb J, Corsa J, Pierdomenico M, Jones K, Olson RE, Macor JE, Albright CF. Meredith JE Jr, et al. J Pharmacol Exp Ther. 2008 Aug;326(2):502-13. doi: 10.1124/jpet.108.138974. Epub 2008 May 22. J Pharmacol Exp Ther. 2008. PMID: 18499745
The amyloid-beta rise and gamma-secretase inhibitor potency depend on the level of substrate expression.
Burton CR, Meredith JE, Barten DM, Goldstein ME, Krause CM, Kieras CJ, Sisk L, Iben LG, Polson C, Thompson MW, Lin XA, Corsa J, Fiedler T, Pierdomenico M, Cao Y, Roach AH, Cantone JL, Ford MJ, Drexler DM, Olson RE, Yang MG, Bergstrom CP, McElhone KE, Bronson JJ, Macor JE, Blat Y, Grafstrom RH, Stern AM, Seiffert DA, Zaczek R, Albright CF, Toyn JH. Burton CR, et al. J Biol Chem. 2008 Aug 22;283(34):22992-3003. doi: 10.1074/jbc.M804175200. Epub 2008 Jun 23. J Biol Chem. 2008. PMID: 18574238 Free article.
Synthesis and SAR of indole-and 7-azaindole-1,3-dicarboxamide hydroxyethylamine inhibitors of BACE-1.
Marcin LR, Higgins MA, Zusi FC, Zhang Y, Dee MF, Parker MF, Muckelbauer JK, Camac DM, Morin PE, Ramamurthy V, Tebben AJ, Lentz KA, Grace JE, Marcinkeviciene JA, Kopcho LM, Burton CR, Barten DM, Toyn JH, Meredith JE, Albright CF, Bronson JJ, Macor JE, Thompson LA. Marcin LR, et al. Among authors: burton cr. Bioorg Med Chem Lett. 2011 Jan 1;21(1):537-41. doi: 10.1016/j.bmcl.2010.10.079. Bioorg Med Chem Lett. 2011. PMID: 21078556
Monosubstituted γ-lactam and conformationally constrained 1,3-diaminopropan-2-ol transition-state isostere inhibitors of β-secretase (BACE).
Boy KM, Guernon JM, Shi J, Toyn JH, Meredith JE, Barten DM, Burton CR, Albright CF, Marcinkeviciene J, Good AC, Tebben AJ, Muckelbauer JK, Camac DM, Lentz KA, Bronson JJ, Olson RE, Macor JE, Thompson LA 3rd. Boy KM, et al. Among authors: burton cr. Bioorg Med Chem Lett. 2011 Nov 15;21(22):6916-24. doi: 10.1016/j.bmcl.2011.06.109. Epub 2011 Jun 30. Bioorg Med Chem Lett. 2011. PMID: 21782431
89 results