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Page 1
De novo fragment design: a medicinal chemistry approach to fragment-based lead generation.
Talamas FX, Ao-Ieong G, Brameld KA, Chin E, de Vicente J, Dunn JP, Ghate M, Giannetti AM, Harris SF, Labadie SS, Leveque V, Li J, Lui AS, McCaleb KL, Nájera I, Schoenfeld RC, Wang B, Wong A. Talamas FX, et al. Among authors: brameld ka. J Med Chem. 2013 Apr 11;56(7):3115-9. doi: 10.1021/jm4002605. Epub 2013 Mar 29. J Med Chem. 2013. PMID: 23509929
Discovery of a novel series of potent non-nucleoside inhibitors of hepatitis C virus NS5B.
Schoenfeld RC, Bourdet DL, Brameld KA, Chin E, de Vicente J, Fung A, Harris SF, Lee EK, Le Pogam S, Leveque V, Li J, Lui AS, Najera I, Rajyaguru S, Sangi M, Steiner S, Talamas FX, Taygerly JP, Zhao J. Schoenfeld RC, et al. Among authors: brameld ka. J Med Chem. 2013 Oct 24;56(20):8163-82. doi: 10.1021/jm401266k. Epub 2013 Oct 10. J Med Chem. 2013. PMID: 24069953 Free PMC article.
Discovery of N-[4-[6-tert-butyl-5-methoxy-8-(6-methoxy-2-oxo-1H-pyridin-3-yl)-3-quinolyl]phenyl]methanesulfonamide (RG7109), a potent inhibitor of the hepatitis C virus NS5B polymerase.
Talamas FX, Abbot SC, Anand S, Brameld KA, Carter DS, Chen J, Davis D, de Vicente J, Fung AD, Gong L, Harris SF, Inbar P, Labadie SS, Lee EK, Lemoine R, Le Pogam S, Leveque V, Li J, McIntosh J, Nájera I, Park J, Railkar A, Rajyaguru S, Sangi M, Schoenfeld RC, Staben LR, Tan Y, Taygerly JP, Villaseñor AG, Weller PE. Talamas FX, et al. Among authors: brameld ka. J Med Chem. 2014 Mar 13;57(5):1914-31. doi: 10.1021/jm401329s. Epub 2013 Nov 6. J Med Chem. 2014. PMID: 24195700 Free PMC article.
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. 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
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. Among authors: brameld ka. 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 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: brameld ka. 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
The Irreversible Covalent Fibroblast Growth Factor Receptor Inhibitor PRN1371 Exhibits Sustained Inhibition of FGFR after Drug Clearance.
Venetsanakos E, Brameld KA, Phan VT, Verner E, Owens TD, Xing Y, Tam D, LaStant J, Leung K, Karr DE, Hill RJ, Gerritsen ME, Goldstein DM, Funk JO, Bradshaw JM. Venetsanakos E, et al. Among authors: brameld ka. Mol Cancer Ther. 2017 Dec;16(12):2668-2676. doi: 10.1158/1535-7163.MCT-17-0309. Epub 2017 Oct 4. Mol Cancer Ther. 2017. PMID: 28978721
Preclinical Efficacy and Anti-Inflammatory Mechanisms of Action of the Bruton Tyrosine Kinase Inhibitor Rilzabrutinib for Immune-Mediated Disease.
Langrish CL, Bradshaw JM, Francesco MR, Owens TD, Xing Y, Shu J, LaStant J, Bisconte A, Outerbridge C, White SD, Hill RJ, Brameld KA, Goldstein DM, Nunn PA. Langrish CL, et al. Among authors: brameld ka. J Immunol. 2021 Apr 1;206(7):1454-1468. doi: 10.4049/jimmunol.2001130. Epub 2021 Mar 5. J Immunol. 2021. PMID: 33674445 Free PMC article.
18 results