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Page 1
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. Among authors: kallan nc. J Med Chem. 2012 Sep 27;55(18):8110-27. doi: 10.1021/jm301024w. Epub 2012 Sep 18. J Med Chem. 2012. PMID: 22934575
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. Among authors: kallan nc. 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. Among authors: kallan nc. 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 of spirocyclic sulfonamides as potent Akt inhibitors with exquisite selectivity against PKA.
Xu R, Banka A, Blake JF, Mitchell IS, Wallace EM, Bencsik JR, Kallan NC, Spencer KL, Gloor SL, Martinson M, Risom T, Gross SD, Morales TH, Wu WI, Vigers GP, Brandhuber BJ, Skelton NJ. Xu R, et al. Among authors: kallan nc. Bioorg Med Chem Lett. 2011 Apr 15;21(8):2335-40. doi: 10.1016/j.bmcl.2011.02.098. Epub 2011 Feb 26. Bioorg Med Chem Lett. 2011. PMID: 21420856
Discovery of a Novel Class of Imidazo[1,2-a]Pyridines with Potent PDGFR Activity and Oral Bioavailability.
Hicken EJ, Marmsater FP, Munson MC, Schlachter ST, Robinson JE, Allen S, Burgess LE, DeLisle RK, Rizzi JP, Topalov GT, Zhao Q, Hicks JM, Kallan NC, Tarlton E, Allen A, Callejo M, Cox A, Rana S, Klopfenstein N, Woessner R, Lyssikatos JP. Hicken EJ, et al. Among authors: kallan nc. ACS Med Chem Lett. 2013 Nov 12;5(1):78-83. doi: 10.1021/ml4003953. eCollection 2014 Jan 9. ACS Med Chem Lett. 2013. PMID: 24900776 Free PMC article.
Spirocyclic β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors: from hit to lowering of cerebrospinal fluid (CSF) amyloid β in a higher species.
Hunt KW, Cook AW, Watts RJ, Clark CT, Vigers G, Smith D, Metcalf AT, Gunawardana IW, Burkard M, Cox AA, Geck Do MK, Dutcher D, Thomas AA, Rana S, Kallan NC, DeLisle RK, Rizzi JP, Regal K, Sammond D, Groneberg R, Siu M, Purkey H, Lyssikatos JP, Marlow A, Liu X, Tang TP. Hunt KW, et al. Among authors: kallan nc. J Med Chem. 2013 Apr 25;56(8):3379-403. doi: 10.1021/jm4002154. Epub 2013 Apr 16. J Med Chem. 2013. PMID: 23537249
A potential therapeutic target for FLT3-ITD AML: PIM1 kinase.
Fathi AT, Arowojolu O, Swinnen I, Sato T, Rajkhowa T, Small D, Marmsater F, Robinson JE, Gross SD, Martinson M, Allen S, Kallan NC, Levis M. Fathi AT, et al. Among authors: kallan nc. Leuk Res. 2012 Feb;36(2):224-31. doi: 10.1016/j.leukres.2011.07.011. Epub 2011 Jul 29. Leuk Res. 2012. PMID: 21802138 Free PMC article.
12 results