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2,3,5-Trisubstituted pyridines as selective AKT inhibitors. Part II: Improved drug-like properties and kinase selectivity from azaindazoles.
Lin H, Yamashita DS, Zeng J, Xie R, Verma S, Luengo JI, Rhodes N, Zhang S, Robell KA, Choudhry AE, Lai Z, Kumar R, Minthorn EA, Brown KK, Heerding DA. Lin H, et al. Among authors: robell ka. Bioorg Med Chem Lett. 2010 Jan 15;20(2):679-83. doi: 10.1016/j.bmcl.2009.11.060. Epub 2009 Nov 20. Bioorg Med Chem Lett. 2010. PMID: 20005102
Tetrasubstituted pyridines as potent and selective AKT inhibitors: Reduced CYP450 and hERG inhibition of aminopyridines.
Lin H, Yamashita DS, Xie R, Zeng J, Wang W, Leber J, Safonov IG, Verma S, Li M, Lafrance L, Venslavsky J, Takata D, Luengo JI, Kahana JA, Zhang S, Robell KA, Levy D, Kumar R, Choudhry AE, Schaber M, Lai Z, Brown BS, Donovan BT, Minthorn EA, Brown KK, Heerding DA. Lin H, et al. Among authors: robell ka. Bioorg Med Chem Lett. 2010 Jan 15;20(2):684-8. doi: 10.1016/j.bmcl.2009.11.061. Epub 2009 Dec 16. Bioorg Med Chem Lett. 2010. PMID: 20006500
Characterization of an Akt kinase inhibitor with potent pharmacodynamic and antitumor activity.
Rhodes N, Heerding DA, Duckett DR, Eberwein DJ, Knick VB, Lansing TJ, McConnell RT, Gilmer TM, Zhang SY, Robell K, Kahana JA, Geske RS, Kleymenova EV, Choudhry AE, Lai Z, Leber JD, Minthorn EA, Strum SL, Wood ER, Huang PS, Copeland RA, Kumar R. Rhodes N, et al. Among authors: robell k. Cancer Res. 2008 Apr 1;68(7):2366-74. doi: 10.1158/0008-5472.CAN-07-5783. Cancer Res. 2008. PMID: 18381444
A non-ATP-competitive inhibitor of BCR-ABL overrides imatinib resistance.
Gumireddy K, Baker SJ, Cosenza SC, John P, Kang AD, Robell KA, Reddy MV, Reddy EP. Gumireddy K, et al. Among authors: robell ka. Proc Natl Acad Sci U S A. 2005 Feb 8;102(6):1992-7. doi: 10.1073/pnas.0408283102. Epub 2005 Jan 27. Proc Natl Acad Sci U S A. 2005. PMID: 15677719 Free PMC article.
Discovery of a clinical stage multi-kinase inhibitor sodium (E)-2-{2-methoxy-5-[(2',4',6'-trimethoxystyrylsulfonyl)methyl]phenylamino}acetate (ON 01910.Na): synthesis, structure-activity relationship, and biological activity.
Reddy MV, Venkatapuram P, Mallireddigari MR, Pallela VR, Cosenza SC, Robell KA, Akula B, Hoffman BS, Reddy EP. Reddy MV, et al. Among authors: robell ka. J Med Chem. 2011 Sep 22;54(18):6254-76. doi: 10.1021/jm200570p. Epub 2011 Aug 17. J Med Chem. 2011. PMID: 21812421 Free PMC article.
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