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Page 1
CC-223, a Potent and Selective Inhibitor of mTOR Kinase: In Vitro and In Vivo Characterization.
Mortensen DS, Fultz KE, Xu S, Xu W, Packard G, Khambatta G, Gamez JC, Leisten J, Zhao J, Apuy J, Ghoreishi K, Hickman M, Narla RK, Bissonette R, Richardson S, Peng SX, Perrin-Ninkovic S, Tran T, Shi T, Yang WQ, Tong Z, Cathers BE, Moghaddam MF, Canan SS, Worland P, Sankar S, Raymon HK. Mortensen DS, et al. Among authors: packard g. Mol Cancer Ther. 2015 Jun;14(6):1295-305. doi: 10.1158/1535-7163.MCT-14-1052. Epub 2015 Apr 8. Mol Cancer Ther. 2015. PMID: 25855786
Discovery of mammalian target of rapamycin (mTOR) kinase inhibitor CC-223.
Mortensen DS, Perrin-Ninkovic SM, Shevlin G, Zhao J, Packard G, Bahmanyar S, Correa M, Elsner J, Harris R, Lee BG, Papa P, Parnes JS, Riggs JR, Sapienza J, Tehrani L, Whitefield B, Apuy J, Bisonette RR, Gamez JC, Hickman M, Khambatta G, Leisten J, Peng SX, Richardson SJ, Cathers BE, Canan SS, Moghaddam MF, Raymon HK, Worland P, Narla RK, Fultz KE, Sankar S. Mortensen DS, et al. Among authors: packard g. J Med Chem. 2015 Jul 9;58(13):5323-33. doi: 10.1021/acs.jmedchem.5b00626. Epub 2015 Jun 26. J Med Chem. 2015. PMID: 26083478
Optimization of a Series of Triazole Containing Mammalian Target of Rapamycin (mTOR) Kinase Inhibitors and the Discovery of CC-115.
Mortensen DS, Perrin-Ninkovic SM, Shevlin G, Elsner J, Zhao J, Whitefield B, Tehrani L, Sapienza J, Riggs JR, Parnes JS, Papa P, Packard G, Lee BG, Harris R, Correa M, Bahmanyar S, Richardson SJ, Peng SX, Leisten J, Khambatta G, Hickman M, Gamez JC, Bisonette RR, Apuy J, Cathers BE, Canan SS, Moghaddam MF, Raymon HK, Worland P, Narla RK, Fultz KE, Sankar S. Mortensen DS, et al. Among authors: packard g. J Med Chem. 2015 Jul 23;58(14):5599-608. doi: 10.1021/acs.jmedchem.5b00627. Epub 2015 Jul 8. J Med Chem. 2015. PMID: 26102506
Discovery and optimization of thieno[2,3-d]pyrimidines as B-Raf inhibitors.
Packard GK, Papa P, Riggs JR, Erdman P, Tehrani L, Robinson D, Harris R, Shevlin G, Perrin-Ninkovic S, Hilgraf R, McCarrick MA, Tran T, Fleming Y, Bai A, Richardson S, Katz J, Tang Y, Leisten J, Moghaddam M, Cathers B, Zhu D, Sakata S. Packard GK, et al. Bioorg Med Chem Lett. 2012 Jan 1;22(1):747-52. doi: 10.1016/j.bmcl.2011.03.006. Epub 2011 Mar 6. Bioorg Med Chem Lett. 2012. PMID: 22137342
Targeting Oncogene mRNA Translation in B-Cell Malignancies with eFT226, a Potent and Selective Inhibitor of eIF4A.
Thompson PA, Eam B, Young NP, Fish S, Chen J, Barrera M, Howard H, Sung E, Parra A, Staunton J, Chiang GG, Gerson-Gurwitz A, Wegerski CJ, Nevarez A, Clarine J, Sperry S, Xiang A, Nilewski C, Packard GK, Michels T, Tran C, Sprengeler PA, Ernst JT, Reich SH, Webster KR. Thompson PA, et al. Among authors: packard gk. Mol Cancer Ther. 2021 Jan;20(1):26-36. doi: 10.1158/1535-7163.MCT-19-0973. Epub 2020 Oct 9. Mol Cancer Ther. 2021. PMID: 33037136
A Novel Triazolopyridine-Based Spleen Tyrosine Kinase Inhibitor That Arrests Joint Inflammation.
Ferguson GD, Delgado M, Plantevin-Krenitsky V, Jensen-Pergakes K, Bates RJ, Torres S, Celeridad M, Brown H, Burnett K, Nadolny L, Tehrani L, Packard G, Pagarigan B, Haelewyn J, Nguyen T, Xu L, Tang Y, Hickman M, Baculi F, Pierce S, Miyazawa K, Jackson P, Chamberlain P, LeBrun L, Xie W, Bennett B, Blease K. Ferguson GD, et al. Among authors: packard g. PLoS One. 2016 Jan 12;11(1):e0145705. doi: 10.1371/journal.pone.0145705. eCollection 2016. PLoS One. 2016. PMID: 26756335 Free PMC article.
Identification of a novel 3,5-disubstituted pyridine as a potent, selective, and orally active inhibitor of Akt1 kinase.
Thomas SA, Li T, Woods KW, Song X, Packard G, Fischer JP, Diebold RB, Liu X, Shi Y, Klinghofer V, Johnson EF, Bouska JJ, Olson A, Guan R, Magnone SR, Marsh K, Luo Y, Rosenberg SH, Giranda VL, Li Q. Thomas SA, et al. Among authors: packard g. Bioorg Med Chem Lett. 2006 Jul 15;16(14):3740-4. doi: 10.1016/j.bmcl.2006.04.046. Epub 2006 May 5. Bioorg Med Chem Lett. 2006. PMID: 16678413
1-Aminomethyl SAR in a novel series of flavagline-inspired eIF4A inhibitors: Effects of amine substitution on cell potency and in vitro PK properties.
Nilewski C, Michels TD, Packard GK, Xiang AX, Sprengeler PA, Eam B, Fish S, Thompson PA, Wegerski CJ, Nevarez A, Clarine J, Sperry S, Ernst JT, Reich SH. Nilewski C, et al. Bioorg Med Chem Lett. 2021 Sep 1;47:128111. doi: 10.1016/j.bmcl.2021.128111. Epub 2021 Aug 2. Bioorg Med Chem Lett. 2021. PMID: 34353608
Design of Development Candidate eFT226, a First in Class Inhibitor of Eukaryotic Initiation Factor 4A RNA Helicase.
Ernst JT, Thompson PA, Nilewski C, Sprengeler PA, Sperry S, Packard G, Michels T, Xiang A, Tran C, Wegerski CJ, Eam B, Young NP, Fish S, Chen J, Howard H, Staunton J, Molter J, Clarine J, Nevarez A, Chiang GG, Appleman JR, Webster KR, Reich SH. Ernst JT, et al. Among authors: packard g. J Med Chem. 2020 Jun 11;63(11):5879-5955. doi: 10.1021/acs.jmedchem.0c00182. Epub 2020 May 29. J Med Chem. 2020. PMID: 32470302
Synthesis and structure-activity relationship of 3,4'-bispyridinylethylenes: discovery of a potent 3-isoquinolinylpyridine inhibitor of protein kinase B (PKB/Akt) for the treatment of cancer.
Li Q, Woods KW, Thomas S, Zhu GD, Packard G, Fisher J, Li T, Gong J, Dinges J, Song X, Abrams J, Luo Y, Johnson EF, Shi Y, Liu X, Klinghofer V, Des Jong R, Oltersdorf T, Stoll VS, Jakob CG, Rosenberg SH, Giranda VL. Li Q, et al. Among authors: packard g. Bioorg Med Chem Lett. 2006 Apr 1;16(7):2000-7. doi: 10.1016/j.bmcl.2005.12.065. Epub 2006 Jan 18. Bioorg Med Chem Lett. 2006. PMID: 16413780
104 results