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Pyridyl-pyrimidine benzimidazole derivatives as potent, selective, and orally bioavailable inhibitors of Tie-2 kinase.
Cee VJ, Cheng AC, Romero K, Bellon S, Mohr C, Whittington DA, Bak A, Bready J, Caenepeel S, Coxon A, Deak HL, Fretland J, Gu Y, Hodous BL, Huang X, Kim JL, Lin J, Long AM, Nguyen H, Olivieri PR, Patel VF, Wang L, Zhou Y, Hughes P, Geuns-Meyer S. Cee VJ, et al. Among authors: nguyen h. Bioorg Med Chem Lett. 2009 Jan 15;19(2):424-7. doi: 10.1016/j.bmcl.2008.11.056. Epub 2008 Nov 20. Bioorg Med Chem Lett. 2009. PMID: 19062275
Discovery of N-(4-(3-(2-aminopyrimidin-4-yl)pyridin-2-yloxy)phenyl)-4-(4-methylthiophen-2-yl)phthalazin-1-amine (AMG 900), a highly selective, orally bioavailable inhibitor of aurora kinases with activity against multidrug-resistant cancer cell lines.
Geuns-Meyer S, Cee VJ, Deak HL, Du B, Hodous BL, Nguyen HN, Olivieri PR, Schenkel LB, Vaida KR, Andrews P, Bak A, Be X, Beltran PJ, Bush TL, Chaves MK, Chung G, Dai Y, Eden P, Hanestad K, Huang L, Lin MH, Tang J, Ziegler B, Radinsky R, Kendall R, Patel VF, Payton M. Geuns-Meyer S, et al. J Med Chem. 2015 Jul 9;58(13):5189-207. doi: 10.1021/acs.jmedchem.5b00183. Epub 2015 May 31. J Med Chem. 2015. PMID: 25970324
Discovery of a potent, selective, and orally bioavailable pyridinyl-pyrimidine phthalazine aurora kinase inhibitor.
Cee VJ, Schenkel LB, Hodous BL, Deak HL, Nguyen HN, Olivieri PR, Romero K, Bak A, Be X, Bellon S, Bush TL, Cheng AC, Chung G, Coats S, Eden PM, Hanestad K, Gallant PL, Gu Y, Huang X, Kendall RL, Lin MH, Morrison MJ, Patel VF, Radinsky R, Rose PE, Ross S, Sun JR, Tang J, Zhao H, Payton M, Geuns-Meyer SD. Cee VJ, et al. Among authors: nguyen hn. J Med Chem. 2010 Sep 9;53(17):6368-77. doi: 10.1021/jm100394y. J Med Chem. 2010. PMID: 20684549
Preclinical evaluation of AMG 900, a novel potent and highly selective pan-aurora kinase inhibitor with activity in taxane-resistant tumor cell lines.
Payton M, Bush TL, Chung G, Ziegler B, Eden P, McElroy P, Ross S, Cee VJ, Deak HL, Hodous BL, Nguyen HN, Olivieri PR, Romero K, Schenkel LB, Bak A, Stanton M, Dussault I, Patel VF, Geuns-Meyer S, Radinsky R, Kendall RL. Payton M, et al. Cancer Res. 2010 Dec 1;70(23):9846-54. doi: 10.1158/0008-5472.CAN-10-3001. Epub 2010 Oct 8. Cancer Res. 2010. PMID: 20935223
Synthesis of 4-substituted chlorophthalazines, dihydrobenzoazepinediones, 2-pyrazolylbenzoic acid, and 2-pyrazolylbenzohydrazide via 3-substituted 3-hydroxyisoindolin-1-ones.
Nguyen HN, Cee VJ, Deak HL, Du B, Faber KP, Gunaydin H, Hodous BL, Hollis SL, Krolikowski PH, Olivieri PR, Patel VF, Romero K, Schenkel LB, Geuns-Meyer SD. Nguyen HN, et al. J Org Chem. 2012 Apr 20;77(8):3887-906. doi: 10.1021/jo3000628. Epub 2012 Apr 5. J Org Chem. 2012. PMID: 22458369
Identification of a potent, state-dependent inhibitor of Nav1.7 with oral efficacy in the formalin model of persistent pain.
Bregman H, Berry L, Buchanan JL, Chen A, Du B, Feric E, Hierl M, Huang L, Immke D, Janosky B, Johnson D, Li X, Ligutti J, Liu D, Malmberg A, Matson D, McDermott J, Miu P, Nguyen HN, Patel VF, Waldon D, Wilenkin B, Zheng XM, Zou A, McDonough SI, DiMauro EF. Bregman H, et al. Among authors: nguyen hn. J Med Chem. 2011 Jul 14;54(13):4427-45. doi: 10.1021/jm200018k. Epub 2011 Jun 2. J Med Chem. 2011. PMID: 21634377
Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency and Pharmacokinetics While Mitigating Metabolic Liabilities.
Weiss MM, Dineen TA, Marx IE, Altmann S, Boezio A, Bregman H, Chu-Moyer M, DiMauro EF, Feric Bojic E, Foti RS, Gao H, Graceffa R, Gunaydin H, Guzman-Perez A, Huang H, Huang L, Jarosh M, Kornecook T, Kreiman CR, Ligutti J, La DS, Lin MJ, Liu D, Moyer BD, Nguyen HN, Peterson EA, Rose PE, Taborn K, Youngblood BD, Yu V, Fremeau RT Jr. Weiss MM, et al. Among authors: nguyen hn. J Med Chem. 2017 Jul 27;60(14):5969-5989. doi: 10.1021/acs.jmedchem.6b01851. Epub 2017 Apr 20. J Med Chem. 2017. PMID: 28287723
Discovery of a biarylamide series of potent, state-dependent NaV1.7 inhibitors.
Schenkel LB, DiMauro EF, Nguyen HN, Chakka N, Du B, Foti RS, Guzman-Perez A, Jarosh M, La DS, Ligutti J, Milgram BC, Moyer BD, Peterson EA, Roberts J, Yu VL, Weiss MM. Schenkel LB, et al. Bioorg Med Chem Lett. 2017 Aug 15;27(16):3817-3824. doi: 10.1016/j.bmcl.2017.06.054. Epub 2017 Jun 26. Bioorg Med Chem Lett. 2017. PMID: 28684121
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