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43 results

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Page 1
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
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
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
Non-oxime pyrazole based inhibitors of B-Raf kinase.
Newhouse BJ, Hansen JD, Grina J, Welch M, Topalov G, Littman N, Callejo M, Martinson M, Galbraith S, Laird ER, Brandhuber BJ, Vigers G, Morales T, Woessner R, Randolph N, Lyssikatos J, Olivero A. Newhouse BJ, et al. Among authors: vigers g. Bioorg Med Chem Lett. 2011 Jun 1;21(11):3488-92. doi: 10.1016/j.bmcl.2010.12.038. Epub 2010 Dec 17. Bioorg Med Chem Lett. 2011. PMID: 21536432
Highly potent and selective 3-N-methylquinazoline-4(3H)-one based inhibitors of B-Raf(V600E) kinase.
Wenglowsky S, Ren L, Grina J, Hansen JD, Laird ER, Moreno D, Dinkel V, Gloor SL, Hastings G, Rana S, Rasor K, Sturgis HL, Voegtli WC, Vigers G, Willis B, Mathieu S, Rudolph J. Wenglowsky S, et al. Among authors: vigers g. Bioorg Med Chem Lett. 2014 Apr 15;24(8):1923-7. doi: 10.1016/j.bmcl.2014.03.007. Epub 2014 Mar 13. Bioorg Med Chem Lett. 2014. PMID: 24675381
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
Discovery and SAR of spirochromane Akt inhibitors.
Kallan NC, Spencer KL, Blake JF, Xu R, Heizer J, Bencsik JR, Mitchell IS, Gloor SL, Martinson M, Risom T, Gross SD, Morales TH, Wu WI, Vigers GP, Brandhuber BJ, Skelton NJ. Kallan NC, et al. Bioorg Med Chem Lett. 2011 Apr 15;21(8):2410-4. doi: 10.1016/j.bmcl.2011.02.073. Epub 2011 Feb 18. Bioorg Med Chem Lett. 2011. PMID: 21392984
Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors.
Blake JF, Xu R, Bencsik JR, Xiao D, Kallan NC, Schlachter S, Mitchell IS, Spencer KL, Banka AL, Wallace EM, Gloor SL, Martinson M, Woessner RD, Vigers GP, Brandhuber BJ, Liang J, Safina BS, Li J, Zhang B, Chabot C, Do S, Lee L, Oeh J, Sampath D, Lee BB, Lin K, Liederer BM, Skelton NJ. Blake JF, et al. J Med Chem. 2012 Sep 27;55(18):8110-27. doi: 10.1021/jm301024w. Epub 2012 Sep 18. J Med Chem. 2012. PMID: 22934575
43 results