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Page 1
Targeting the Mitotic Kinesin KIF18A in Chromosomally Unstable Cancers: Hit Optimization Toward an In Vivo Chemical Probe.
Tamayo NA, Bourbeau MP, Allen JR, Ashton KS, Chen JJ, Kaller MR, Nguyen TT, Nishimura N, Pettus LH, Walton M, Belmontes B, Moriguchi J, Chen K, McCarter JD, Hanestad K, Chung G, Ninniri MSS, Sun J, Poppe L, Spahr C, Hui J, Jia L, Wu T, Dahal UP, Edson KZ, Payton M. Tamayo NA, et al. Among authors: nguyen tt. J Med Chem. 2022 Mar 24;65(6):4972-4990. doi: 10.1021/acs.jmedchem.1c02030. Epub 2022 Mar 14. J Med Chem. 2022. PMID: 35286090
Design and synthesis of quinolin-2(1H)-one derivatives as potent CDK5 inhibitors.
Zhong W, Liu H, Kaller MR, Henley C, Magal E, Nguyen T, Osslund TD, Powers D, Rzasa RM, Wang HL, Wang W, Xiong X, Zhang J, Norman MH. Zhong W, et al. Bioorg Med Chem Lett. 2007 Oct 1;17(19):5384-9. doi: 10.1016/j.bmcl.2007.07.045. Epub 2007 Aug 6. Bioorg Med Chem Lett. 2007. PMID: 17709247
Design and synthesis of 6-oxo-1,6-dihydropyridines as CDK5 inhibitors.
Kaller MR, Zhong W, Henley C, Magal E, Nguyen T, Powers D, Rzasa RM, Wang W, Xiong X, Norman MH. Kaller MR, et al. Bioorg Med Chem Lett. 2009 Dec 1;19(23):6591-4. doi: 10.1016/j.bmcl.2009.10.027. Epub 2009 Oct 13. Bioorg Med Chem Lett. 2009. PMID: 19864130
3-Oxo-2-piperazinyl acetamides as potent bradykinin B1 receptor antagonists for the treatment of pain and inflammation.
Chen JJ, Nguyen T, D'Amico DC, Qian W, Human J, Aya T, Biswas K, Fotsch C, Han N, Liu Q, Nishimura N, Peterkin TA, Yang K, Zhu J, Riahi BB, Hungate RW, Andersen NG, Colyer JT, Faul MM, Kamassah A, Wang J, Jona J, Kumar G, Johnson E, Askew BC. Chen JJ, et al. Bioorg Med Chem Lett. 2011 Jun 1;21(11):3384-9. doi: 10.1016/j.bmcl.2011.03.115. Epub 2011 Apr 7. Bioorg Med Chem Lett. 2011. PMID: 21514825
Design and preparation of a potent series of hydroxyethylamine containing β-secretase inhibitors that demonstrate robust reduction of central β-amyloid.
Weiss MM, Williamson T, Babu-Khan S, Bartberger MD, Brown J, Chen K, Cheng Y, Citron M, Croghan MD, Dineen TA, Esmay J, Graceffa RF, Harried SS, Hickman D, Hitchcock SA, Horne DB, Huang H, Imbeah-Ampiah R, Judd T, Kaller MR, Kreiman CR, La DS, Li V, Lopez P, Louie S, Monenschein H, Nguyen TT, Pennington LD, Rattan C, San Miguel T, Sickmier EA, Wahl RC, Wen PH, Wood S, Xue Q, Yang BH, Patel VF, Zhong W. Weiss MM, et al. Among authors: nguyen tt. J Med Chem. 2012 Nov 8;55(21):9009-24. doi: 10.1021/jm300119p. Epub 2012 Apr 18. J Med Chem. 2012. PMID: 22468639
Design and synthesis of potent, orally efficacious hydroxyethylamine derived β-site amyloid precursor protein cleaving enzyme (BACE1) inhibitors.
Dineen TA, Weiss MM, Williamson T, Acton P, Babu-Khan S, Bartberger MD, Brown J, Chen K, Cheng Y, Citron M, Croghan MD, Dunn RT 2nd, Esmay J, Graceffa RF, Harried SS, Hickman D, Hitchcock SA, Horne DB, Huang H, Imbeah-Ampiah R, Judd T, Kaller MR, Kreiman CR, La DS, Li V, Lopez P, Louie S, Monenschein H, Nguyen TT, Pennington LD, San Miguel T, Sickmier EA, Vargas HM, Wahl RC, Wen PH, Whittington DA, Wood S, Xue Q, Yang BH, Patel VF, Zhong W. Dineen TA, et al. Among authors: nguyen tt. J Med Chem. 2012 Nov 8;55(21):9025-44. doi: 10.1021/jm300118s. Epub 2012 Apr 18. J Med Chem. 2012. PMID: 22468684
Hydroxyethylamine-based inhibitors of BACE1: P₁-P₃ macrocyclization can improve potency, selectivity, and cell activity.
Pennington LD, Whittington DA, Bartberger MD, Jordan SR, Monenschein H, Nguyen TT, Yang BH, Xue QM, Vounatsos F, Wahl RC, Chen K, Wood S, Citron M, Patel VF, Hitchcock SA, Zhong W. Pennington LD, et al. Among authors: nguyen tt. Bioorg Med Chem Lett. 2013 Aug 1;23(15):4459-64. doi: 10.1016/j.bmcl.2013.05.028. Epub 2013 May 16. Bioorg Med Chem Lett. 2013. PMID: 23769639
Optimization of potency and pharmacokinetic properties of tetrahydroisoquinoline transient receptor potential melastatin 8 (TRPM8) antagonists.
Horne DB, Tamayo NA, Bartberger MD, Bo Y, Clarine J, Davis CD, Gore VK, Kaller MR, Lehto SG, Ma VV, Nishimura N, Nguyen TT, Tang P, Wang W, Youngblood BD, Zhang M, Gavva NR, Monenschein H, Norman MH. Horne DB, et al. Among authors: nguyen tt. J Med Chem. 2014 Apr 10;57(7):2989-3004. doi: 10.1021/jm401955h. Epub 2014 Mar 19. J Med Chem. 2014. PMID: 24597733
A Potent and Orally Efficacious, Hydroxyethylamine-Based Inhibitor of β-Secretase.
Kaller MR, Harried SS, Albrecht B, Amarante P, Babu-Khan S, Bartberger MD, Brown J, Brown R, Chen K, Cheng Y, Citron M, Croghan MD, Graceffa R, Hickman D, Judd T, Kriemen C, La D, Li V, Lopez P, Luo Y, Masse C, Monenschein H, Nguyen T, Pennington LD, Miguel TS, Sickmier EA, Wahl RC, Weiss MM, Wen PH, Williamson T, Wood S, Xue M, Yang B, Zhang J, Patel V, Zhong W, Hitchcock S. Kaller MR, et al. ACS Med Chem Lett. 2012 Mar 29;3(11):886-91. doi: 10.1021/ml3000148. eCollection 2012 Nov 8. ACS Med Chem Lett. 2012. PMID: 24900403 Free PMC article.
4,332 results