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Page 1
8-Tetrahydropyran-2-yl chromans: highly selective beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors.
Thomas AA, Hunt KW, Newhouse B, Watts RJ, Liu X, Vigers G, Smith D, Rhodes SP, Brown KD, Otten JN, Burkard M, Cox AA, Geck Do MK, Dutcher D, Rana S, DeLisle RK, Regal K, Wright AD, Groneberg R, Liao J, Scearce-Levie K, Siu M, Purkey HE, Lyssikatos JP. Thomas AA, et al. Among authors: vigers g. J Med Chem. 2014 Dec 11;57(23):10112-29. doi: 10.1021/jm5015132. Epub 2014 Nov 26. J Med Chem. 2014. PMID: 25411915
Potent selective nonpeptidic inhibitors of human lung tryptase.
Burgess LE, Newhouse BJ, Ibrahim P, Rizzi J, Kashem MA, Hartman A, Brandhuber BJ, Wright CD, Thomson DS, Vigers GP, Koch K. Burgess LE, et al. Among authors: vigers gp. Proc Natl Acad Sci U S A. 1999 Jul 20;96(15):8348-52. doi: 10.1073/pnas.96.15.8348. Proc Natl Acad Sci U S A. 1999. PMID: 10411878 Free PMC article.
Non-charged thiamine analogs as inhibitors of enzyme transketolase.
Thomas AA, De Meese J, Le Huerou Y, Boyd SA, Romoff TT, Gonzales SS, Gunawardana I, Kaplan T, Sullivan F, Condroski K, Lyssikatos JP, Aicher TD, Ballard J, Bernat B, DeWolf W, Han M, Lemieux C, Smith D, Weiler S, Wright SK, Vigers G, Brandhuber B. Thomas AA, et al. Among authors: vigers g. Bioorg Med Chem Lett. 2008 Jan 15;18(2):509-12. doi: 10.1016/j.bmcl.2007.11.098. Epub 2007 Dec 3. Bioorg Med Chem Lett. 2008. PMID: 18182286
Synthesis, in vitro and in vivo activity of thiamine antagonist transketolase inhibitors.
Thomas AA, Le Huerou Y, De Meese J, Gunawardana I, Kaplan T, Romoff TT, Gonzales SS, Condroski K, Boyd SA, Ballard J, Bernat B, DeWolf W, Han M, Lee P, Lemieux C, Pedersen R, Pheneger J, Poch G, Smith D, Sullivan F, Weiler S, Wright SK, Lin J, Brandhuber B, Vigers G. Thomas AA, et al. Among authors: vigers g. Bioorg Med Chem Lett. 2008 Mar 15;18(6):2206-10. doi: 10.1016/j.bmcl.2007.11.101. Epub 2007 Dec 3. Bioorg Med Chem Lett. 2008. PMID: 18267359
Potent and selective pyrazole-based inhibitors of B-Raf kinase.
Hansen JD, Grina J, Newhouse B, Welch M, Topalov G, Littman N, Callejo M, Gloor S, Martinson M, Laird E, Brandhuber BJ, Vigers G, Morales T, Woessner R, Randolph N, Lyssikatos J, Olivero A. Hansen JD, et al. Among authors: vigers g. Bioorg Med Chem Lett. 2008 Aug 15;18(16):4692-5. doi: 10.1016/j.bmcl.2008.07.002. Epub 2008 Jul 5. Bioorg Med Chem Lett. 2008. PMID: 18676143
Discovery of pyrrolopyrimidine inhibitors of Akt.
Blake JF, Kallan NC, Xiao D, Xu R, Bencsik JR, Skelton NJ, Spencer KL, Mitchell IS, Woessner RD, Gloor SL, Risom T, Gross SD, Martinson M, Morales TH, Vigers GP, Brandhuber BJ. Blake JF, et al. Bioorg Med Chem Lett. 2010 Oct 1;20(19):5607-12. doi: 10.1016/j.bmcl.2010.08.053. Epub 2010 Aug 13. Bioorg Med Chem Lett. 2010. PMID: 20810279
Discovery of dihydrothieno- and dihydrofuropyrimidines as potent pan Akt inhibitors.
Bencsik JR, Xiao D, Blake JF, Kallan NC, Mitchell IS, Spencer KL, Xu R, Gloor SL, Martinson M, Risom T, Woessner RD, Dizon F, Wu WI, Vigers GP, Brandhuber BJ, Skelton NJ, Prior WW, Murray LJ. Bencsik JR, et al. Bioorg Med Chem Lett. 2010 Dec 1;20(23):7037-41. doi: 10.1016/j.bmcl.2010.09.112. Epub 2010 Sep 29. Bioorg Med Chem Lett. 2010. PMID: 20971641
The discovery of furo[2,3-c]pyridine-based indanone oximes as potent and selective B-Raf inhibitors.
Buckmelter AJ, Ren L, Laird ER, Rast B, Miknis G, Wenglowsky S, Schlachter S, Welch M, Tarlton E, Grina J, Lyssikatos J, Brandhuber BJ, Morales T, Randolph N, Vigers G, Martinson M, Callejo M. Buckmelter AJ, et al. Among authors: vigers g. Bioorg Med Chem Lett. 2011 Feb 15;21(4):1248-52. doi: 10.1016/j.bmcl.2010.12.039. Epub 2010 Dec 10. Bioorg Med Chem Lett. 2011. PMID: 21211972
Non-oxime inhibitors of B-Raf(V600E) kinase.
Ren L, Wenglowsky S, Miknis G, Rast B, Buckmelter AJ, Ely RJ, Schlachter S, Laird ER, Randolph N, Callejo M, Martinson M, Galbraith S, Brandhuber BJ, Vigers G, Morales T, Voegtli WC, Lyssikatos J. Ren L, et al. Among authors: vigers g. Bioorg Med Chem Lett. 2011 Feb 15;21(4):1243-7. doi: 10.1016/j.bmcl.2010.12.061. Epub 2010 Dec 19. Bioorg Med Chem Lett. 2011. PMID: 21251822
43 results