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Page 1
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: arcalas a. 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
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. Among authors: arcalas a. 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. Among authors: arcalas a. 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 of XL888: a novel tropane-derived small molecule inhibitor of HSP90.
Bussenius J, Blazey CM, Aay N, Anand NK, Arcalas A, Baik T, Bowles OJ, Buhr CA, Costanzo S, Curtis JK, DeFina SC, Dubenko L, Heuer TS, Huang P, Jaeger C, Joshi A, Kennedy AR, Kim AI, Lara K, Lee J, Li J, Lougheed JC, Ma S, Malek S, Manalo JC, Martini JF, McGrath G, Nicoll M, Nuss JM, Pack M, Peto CJ, Tsang TH, Wang L, Womble SW, Yakes M, Zhang W, Rice KD. Bussenius J, et al. Among authors: arcalas a. Bioorg Med Chem Lett. 2012 Sep 1;22(17):5396-404. doi: 10.1016/j.bmcl.2012.07.052. Epub 2012 Jul 21. Bioorg Med Chem Lett. 2012. PMID: 22877636
Discovery of a novel class of highly potent, selective, ATP-competitive, and orally bioavailable inhibitors of the mammalian target of rapamycin (mTOR).
Takeuchi CS, Kim BG, Blazey CM, Ma S, Johnson HW, Anand NK, Arcalas A, Baik TG, Buhr CA, Cannoy J, Epshteyn S, Joshi A, Lara K, Lee MS, Wang L, Leahy JW, Nuss JM, Aay N, Aoyama R, Foster P, Lee J, Lehoux I, Munagala N, Plonowski A, Rajan S, Woolfrey J, Yamaguchi K, Lamb P, Miller N. Takeuchi CS, et al. Among authors: arcalas a. J Med Chem. 2013 Mar 28;56(6):2218-34. doi: 10.1021/jm3007933. Epub 2013 Mar 7. J Med Chem. 2013. PMID: 23394126
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. Among authors: arcalas a. J Med Chem. 2012 May 10;55(9):4322-35. doi: 10.1021/jm300122u. Epub 2012 Apr 19. J Med Chem. 2012. PMID: 22497444