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SAR and in vivo evaluation of 4-aryl-2-aminoalkylpyrimidines as potent and selective Janus kinase 2 (JAK2) inhibitors.
Forsyth T, Kearney PC, Kim BG, Johnson HW, Aay N, Arcalas A, Brown DS, Chan V, Chen J, Du H, Epshteyn S, Galan AA, Huynh TP, Ibrahim MA, Kane B, Koltun ES, Mann G, Meyr LE, Lee MS, Lewis GL, Noguchi RT, Pack M, Ridgway BH, Shi X, Takeuchi CS, Zu P, Leahy JW, Nuss JM, Aoyama R, Engst S, Gendreau SB, Kassees R, Li J, Lin SH, Martini JF, Stout T, Tong P, Woolfrey J, Zhang W, Yu P. Forsyth T, et al. Among authors: galan aa. Bioorg Med Chem Lett. 2012 Dec 15;22(24):7653-8. doi: 10.1016/j.bmcl.2012.10.007. Epub 2012 Oct 16. Bioorg Med Chem Lett. 2012. PMID: 23127890
Discovery of a new class of glucosylceramide synthase inhibitors.
Koltun E, Richards S, Chan V, Nachtigall J, Du H, Noson K, Galan A, Aay N, Hanel A, Harrison A, Zhang J, Won KA, Tam D, Qian F, Wang T, Finn P, Ogilvie K, Rosen J, Mohan R, Larson C, Lamb P, Nuss J, Kearney P. Koltun E, et al. Bioorg Med Chem Lett. 2011 Nov 15;21(22):6773-7. doi: 10.1016/j.bmcl.2011.09.037. Epub 2011 Sep 17. Bioorg Med Chem Lett. 2011. PMID: 21974949
The design, synthesis, and biological evaluation of PIM kinase inhibitors.
Tsuhako AL, Brown DS, Koltun ES, Aay N, Arcalas A, Chan V, Du H, Engst S, Franzini M, Galan A, Huang P, Johnston S, Kane B, Kim MH, Laird AD, Lin R, Mock L, Ngan I, Pack M, Stott G, Stout TJ, Yu P, Zaharia C, Zhang W, Zhou P, Nuss JM, Kearney PC, Xu W. Tsuhako AL, et al. Bioorg Med Chem Lett. 2012 Jun 1;22(11):3732-8. doi: 10.1016/j.bmcl.2012.04.025. Epub 2012 Apr 11. Bioorg Med Chem Lett. 2012. PMID: 22542012
Discovery of XL413, a potent and selective CDC7 inhibitor.
Koltun ES, Tsuhako AL, Brown DS, Aay N, Arcalas A, Chan V, Du H, Engst S, Ferguson K, Franzini M, Galan A, Holst CR, Huang P, Kane B, Kim MH, Li J, Markby D, Mohan M, Noson K, Plonowski A, Richards SJ, Robertson S, Shaw K, Stott G, Stout TJ, Young J, Yu P, Zaharia CA, Zhang W, Zhou P, Nuss JM, Xu W, Kearney PC. Koltun ES, et al. Bioorg Med Chem Lett. 2012 Jun 1;22(11):3727-31. doi: 10.1016/j.bmcl.2012.04.024. Epub 2012 Apr 16. Bioorg Med Chem Lett. 2012. PMID: 22560567
Discovery and characterization of an inhibitor of glucosylceramide synthase.
Richards S, Larson CJ, Koltun ES, Hanel A, Chan V, Nachtigall J, Harrison A, Aay N, Du H, Arcalas A, Galan A, Zhang J, Zhang W, Won KA, Tam D, Qian F, Wang T, Finn P, Ogilvie K, Rosen J, Aoyama R, Plonowski A, Cancilla B, Bentzien F, Yakes M, Mohan R, Lamb P, Nuss J, Kearney P. Richards S, et al. J Med Chem. 2012 May 10;55(9):4322-35. doi: 10.1021/jm300122u. Epub 2012 Apr 19. J Med Chem. 2012. PMID: 22497444