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Discovery of Potent and Orally Bioavailable Pyridine N-Oxide-Based Factor XIa Inhibitors through Exploiting Nonclassical Interactions.
Xu G, Liu Z, Wang X, Lu T, DesJarlais RL, Thieu T, Zhang J, Devine ZH, Du F, Li Q, Milligan CM, Shaffer P, Cedervall PE, Spurlino JC, Stratton CF, Pietrak B, Szewczuk LM, Wong V, Steele RA, Bruinzeel W, Chintala M, Silva J, Gaul MD, Macielag MJ, Nargund R. Xu G, et al. Among authors: thieu t. J Med Chem. 2022 Aug 11;65(15):10419-10440. doi: 10.1021/acs.jmedchem.2c00442. Epub 2022 Jul 21. J Med Chem. 2022. PMID: 35862732
2,7-Pyrrolo[2,1-f][1,2,4]triazines as JAK2 inhibitors: modification of target structure to minimize reactive metabolite formation.
Weinberg LR, Albom MS, Angeles TS, Breslin HJ, Gingrich DE, Huang Z, Lisko JG, Mason JL, Milkiewicz KL, Thieu TV, Underiner TL, Wells GJ, Wells-Knecht KJ, Dorsey BD. Weinberg LR, et al. Bioorg Med Chem Lett. 2011 Dec 15;21(24):7325-30. doi: 10.1016/j.bmcl.2011.10.032. Epub 2011 Oct 14. Bioorg Med Chem Lett. 2011. PMID: 22041060
Strategies to mitigate the bioactivation of 2-anilino-7-aryl-pyrrolo[2,1-f][1,2,4]triazines: identification of orally bioavailable, efficacious ALK inhibitors.
Mesaros EF, Thieu TV, Wells GJ, Zificsak CA, Wagner JC, Breslin HJ, Tripathy R, Diebold JL, McHugh RJ, Wohler AT, Quail MR, Wan W, Lu L, Huang Z, Albom MS, Angeles TS, Wells-Knecht KJ, Aimone LD, Cheng M, Ator MA, Ott GR, Dorsey BD. Mesaros EF, et al. Among authors: thieu tv. J Med Chem. 2012 Jan 12;55(1):115-25. doi: 10.1021/jm2010767. Epub 2011 Dec 29. J Med Chem. 2012. PMID: 22141319
2,7-disubstituted-pyrrolo[2,1-f][1,2,4]triazines: new variant of an old template and application to the discovery of anaplastic lymphoma kinase (ALK) inhibitors with in vivo antitumor activity.
Ott GR, Wells GJ, Thieu TV, Quail MR, Lisko JG, Mesaros EF, Gingrich DE, Ghose AK, Wan W, Lu L, Cheng M, Albom MS, Angeles TS, Huang Z, Aimone LD, Ator MA, Ruggeri BA, Dorsey BD. Ott GR, et al. J Med Chem. 2011 Sep 22;54(18):6328-41. doi: 10.1021/jm200758k. Epub 2011 Aug 22. J Med Chem. 2011. PMID: 21859094
Optimization of a novel kinase inhibitor scaffold for the dual inhibition of JAK2 and FAK kinases.
Zificsak CA, Gingrich DE, Breslin HJ, Dunn DD, Milkiewicz KL, Theroff JP, Thieu TV, Underiner TL, Weinberg LR, Aimone LD, Albom MS, Mason JL, Saville L, Husten J, Angeles TS, Finn JP, Jan M, O'Kane TM, Dobrzanski P, Dorsey BD. Zificsak CA, et al. Bioorg Med Chem Lett. 2012 Jan 1;22(1):133-7. doi: 10.1016/j.bmcl.2011.11.049. Epub 2011 Nov 25. Bioorg Med Chem Lett. 2012. PMID: 22169263
7-fluoroindazoles as potent and selective inhibitors of factor Xa.
Lee YK, Parks DJ, Lu T, Thieu TV, Markotan T, Pan W, McComsey DF, Milkiewicz KL, Crysler CS, Ninan N, Abad MC, Giardino EC, Maryanoff BE, Damiano BP, Player MR. Lee YK, et al. Among authors: thieu tv. J Med Chem. 2008 Jan 24;51(2):282-97. doi: 10.1021/jm701217r. Epub 2007 Dec 27. J Med Chem. 2008. PMID: 18159923
Overview of approaches to estimate real-world disease progression in lung cancer.
Amorrortu R, Garcia M, Zhao Y, El Naqa I, Balagurunathan Y, Chen DT, Thieu T, Schabath MB, Rollison DE. Amorrortu R, et al. Among authors: thieu t. JNCI Cancer Spectr. 2023 Oct 31;7(6):pkad074. doi: 10.1093/jncics/pkad074. JNCI Cancer Spectr. 2023. PMID: 37738580 Free PMC article. Review.
29 results