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Page 1
Quinolones as HCV NS5B polymerase inhibitors.
Kumar DV, Rai R, Brameld KA, Somoza JR, Rajagopalan R, Janc JW, Xia YM, Ton TL, Shaghafi MB, Hu H, Lehoux I, To N, Young WB, Green MJ. Kumar DV, et al. Bioorg Med Chem Lett. 2011 Jan 1;21(1):82-7. doi: 10.1016/j.bmcl.2010.11.068. Epub 2010 Nov 21. Bioorg Med Chem Lett. 2011. PMID: 21145235
3-heterocyclyl quinolone inhibitors of the HCV NS5B polymerase.
Kumar DV, Rai R, Brameld KA, Riggs J, Somoza JR, Rajagopalan R, Janc JW, Xia YM, Ton TL, Hu H, Lehoux I, Ho JD, Young WB, Hart B, Green MJ. Kumar DV, et al. Bioorg Med Chem Lett. 2012 Jan 1;22(1):300-4. doi: 10.1016/j.bmcl.2011.11.013. Epub 2011 Nov 9. Bioorg Med Chem Lett. 2012. PMID: 22119470
Discovery of the Irreversible Covalent FGFR Inhibitor 8-(3-(4-Acryloylpiperazin-1-yl)propyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (PRN1371) for the Treatment of Solid Tumors.
Brameld KA, Owens TD, Verner E, Venetsanakos E, Bradshaw JM, Phan VT, Tam D, Leung K, Shu J, LaStant J, Loughhead DG, Ton T, Karr DE, Gerritsen ME, Goldstein DM, Funk JO. Brameld KA, et al. Among authors: ton t. J Med Chem. 2017 Aug 10;60(15):6516-6527. doi: 10.1021/acs.jmedchem.7b00360. Epub 2017 Jul 25. J Med Chem. 2017. PMID: 28665128
Discovery of Reversible Covalent Bruton's Tyrosine Kinase Inhibitors PRN473 and PRN1008 (Rilzabrutinib).
Owens TD, Brameld KA, Verner EJ, Ton T, Li X, Zhu J, Masjedizadeh MR, Bradshaw JM, Hill RJ, Tam D, Bisconte A, Kim EO, Francesco M, Xing Y, Shu J, Karr D, LaStant J, Finkle D, Loewenstein N, Haberstock-Debic H, Taylor MJ, Nunn P, Langrish CL, Goldstein DM. Owens TD, et al. Among authors: ton t. J Med Chem. 2022 Apr 14;65(7):5300-5316. doi: 10.1021/acs.jmedchem.1c01170. Epub 2022 Mar 18. J Med Chem. 2022. PMID: 35302767
Discovery of novel heterocyclic factor VIIa inhibitors.
Rai R, Kolesnikov A, Sprengeler PA, Torkelson S, Ton T, Katz BA, Yu C, Hendrix J, Shrader WD, Stephens R, Cabuslay R, Sanford E, Young WB. Rai R, et al. Among authors: ton t. Bioorg Med Chem Lett. 2006 Apr 15;16(8):2270-3. doi: 10.1016/j.bmcl.2006.01.017. Epub 2006 Feb 3. Bioorg Med Chem Lett. 2006. PMID: 16460932
Efforts toward oral bioavailability in factor VIIa inhibitors.
Vijaykumar D, Rai R, Shaghafi M, Ton T, Torkelson S, Leahy EM, Riggs JR, Hu H, Sprengeler PA, Shrader WD, O'Bryan C, Cabuslay R, Sanford E, Gjerstadt E, Liu L, Sukbuntherng J, Young WB. Vijaykumar D, et al. Among authors: ton t. Bioorg Med Chem Lett. 2006 Jul 15;16(14):3829-32. doi: 10.1016/j.bmcl.2006.04.018. Epub 2006 May 2. Bioorg Med Chem Lett. 2006. PMID: 16650987
Factor VIIa inhibitors: gaining selectivity within the trypsin family.
Shrader WD, Kolesnikov A, Burgess-Henry J, Rai R, Hendrix J, Hu H, Torkelson S, Ton T, Young WB, Katz BA, Yu C, Tang J, Cabuslay R, Sanford E, Janc JW, Sprengeler PA. Shrader WD, et al. Among authors: ton t. Bioorg Med Chem Lett. 2006 Mar 15;16(6):1596-600. doi: 10.1016/j.bmcl.2005.12.040. Epub 2006 Jan 18. Bioorg Med Chem Lett. 2006. PMID: 16413783
Prolonged and tunable residence time using reversible covalent kinase inhibitors.
Bradshaw JM, McFarland JM, Paavilainen VO, Bisconte A, Tam D, Phan VT, Romanov S, Finkle D, Shu J, Patel V, Ton T, Li X, Loughhead DG, Nunn PA, Karr DE, Gerritsen ME, Funk JO, Owens TD, Verner E, Brameld KA, Hill RJ, Goldstein DM, Taunton J. Bradshaw JM, et al. Among authors: ton t. Nat Chem Biol. 2015 Jul;11(7):525-31. doi: 10.1038/nchembio.1817. Epub 2015 May 25. Nat Chem Biol. 2015. PMID: 26006010 Free PMC article.
Passive infusion of an S2-Stem broadly neutralizing antibody protects against SARS-CoV-2 infection and lower airway inflammation in rhesus macaques.
Edwards CT, Karunakaran KA, Garcia E, Beutler N, Gagne M, Golden N, Aoued H, Pellegrini KL, Burnett MR, Honeycutt CC, Lapp SA, Ton T, Lin MC, Metz A, Bombin A, Goff K, Scheuermann SE, Wilkes A, Wood JS, Ehnert S, Weissman S, Curran EH, Roy M, Dessasau E, Paiardini M, Upadhyay AA, Moore IN, Maness NJ, Douek DC, Piantadosi A, Andrabi R, Rogers TR, Burton DR, Bosinger SE. Edwards CT, et al. Among authors: ton t. PLoS Pathog. 2025 Jan 23;21(1):e1012456. doi: 10.1371/journal.ppat.1012456. Online ahead of print. PLoS Pathog. 2025. PMID: 39847599 Free article.
189 results