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Page 1
2,4-Diaminoquinazolines as Dual Toll-like Receptor (TLR) 7/8 Modulators for the Treatment of Hepatitis B Virus.
Embrechts W, Herschke F, Pauwels F, Stoops B, Last S, Pieters S, Pande V, Pille G, Amssoms K, Smyej I, Dhuyvetter D, Scholliers A, Mostmans W, Van Dijck K, Van Schoubroeck B, Thone T, De Pooter D, Fanning G, Jonckers THM, Horton H, Raboisson P, McGowan D. Embrechts W, et al. Among authors: last s. J Med Chem. 2018 Jul 26;61(14):6236-6246. doi: 10.1021/acs.jmedchem.8b00643. Epub 2018 Jul 17. J Med Chem. 2018. PMID: 29965759
1,5-Benzodiazepine inhibitors of HCV NS5B polymerase.
McGowan D, Nyanguile O, Cummings MD, Vendeville S, Vandyck K, Van den Broeck W, Boutton CW, De Bondt H, Quirynen L, Amssoms K, Bonfanti JF, Last S, Rombauts K, Tahri A, Hu L, Delouvroy F, Vermeiren K, Vandercruyssen G, Van der Helm L, Cleiren E, Mostmans W, Lory P, Pille G, Van Emelen K, Fanning G, Pauwels F, Lin TI, Simmen K, Raboisson P. McGowan D, et al. Among authors: last s. Bioorg Med Chem Lett. 2009 May 1;19(9):2492-6. doi: 10.1016/j.bmcl.2009.03.035. Epub 2009 Mar 14. Bioorg Med Chem Lett. 2009. PMID: 19342234
Structure-based macrocyclization yields hepatitis C virus NS5B inhibitors with improved binding affinities and pharmacokinetic properties.
Cummings MD, Lin TI, Hu L, Tahri A, McGowan D, Amssoms K, Last S, Devogelaere B, Rouan MC, Vijgen L, Berke JM, Dehertogh P, Fransen E, Cleiren E, van der Helm L, Fanning G, Van Emelen K, Nyanguile O, Simmen K, Raboisson P, Vendeville S. Cummings MD, et al. Among authors: last s. Angew Chem Int Ed Engl. 2012 May 7;51(19):4637-40. doi: 10.1002/anie.201200110. Epub 2012 Mar 30. Angew Chem Int Ed Engl. 2012. PMID: 22473861 No abstract available.
Finger-loop inhibitors of the HCV NS5b polymerase. Part 1: Discovery and optimization of novel 1,6- and 2,6-macrocyclic indole series.
McGowan D, Vendeville S, Lin TI, Tahri A, Hu L, Cummings MD, Amssoms K, Berke JM, Canard M, Cleiren E, Dehertogh P, Last S, Fransen E, Van Der Helm E, Van den Steen I, Vijgen L, Rouan MC, Fanning G, Nyanguile O, Van Emelen K, Simmen K, Raboisson P. McGowan D, et al. Among authors: last s. Bioorg Med Chem Lett. 2012 Jul 1;22(13):4431-6. doi: 10.1016/j.bmcl.2012.03.097. Epub 2012 Apr 3. Bioorg Med Chem Lett. 2012. PMID: 22542193
Finger loop inhibitors of the HCV NS5b polymerase. Part II. Optimization of tetracyclic indole-based macrocycle leading to the discovery of TMC647055.
Vendeville S, Lin TI, Hu L, Tahri A, McGowan D, Cummings MD, Amssoms K, Canard M, Last S, Van den Steen I, Devogelaere B, Rouan MC, Vijgen L, Berke JM, Dehertogh P, Fransen E, Cleiren E, van der Helm L, Fanning G, Van Emelen K, Nyanguile O, Simmen K, Raboisson P. Vendeville S, et al. Among authors: last s. Bioorg Med Chem Lett. 2012 Jul 1;22(13):4437-43. doi: 10.1016/j.bmcl.2012.04.113. Epub 2012 Apr 30. Bioorg Med Chem Lett. 2012. PMID: 22633687
Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
Cummings MD, Lin TI, Hu L, Tahri A, McGowan D, Amssoms K, Last S, Devogelaere B, Rouan MC, Vijgen L, Berke JM, Dehertogh P, Fransen E, Cleiren E, van der Helm L, Fanning G, Nyanguile O, Simmen K, Van Remoortere P, Raboisson P, Vendeville S. Cummings MD, et al. Among authors: last s. J Med Chem. 2014 Mar 13;57(5):1880-92. doi: 10.1021/jm401396p. Epub 2013 Nov 8. J Med Chem. 2014. PMID: 24144360
Novel Pyrimidine Toll-like Receptor 7 and 8 Dual Agonists to Treat Hepatitis B Virus.
McGowan D, Herschke F, Pauwels F, Stoops B, Last S, Pieters S, Scholliers A, Thoné T, Van Schoubroeck B, De Pooter D, Mostmans W, Khamlichi MD, Embrechts W, Dhuyvetter D, Smyej I, Arnoult E, Demin S, Borghys H, Fanning G, Vlach J, Raboisson P. McGowan D, et al. Among authors: last s. J Med Chem. 2016 Sep 8;59(17):7936-49. doi: 10.1021/acs.jmedchem.6b00747. Epub 2016 Aug 23. J Med Chem. 2016. PMID: 27513093
Identification and Optimization of Pyrrolo[3,2-d]pyrimidine Toll-like Receptor 7 (TLR7) Selective Agonists for the Treatment of Hepatitis B.
McGowan DC, Herschke F, Pauwels F, Stoops B, Smyej I, Last S, Pieters S, Embrechts W, Khamlichi MD, Thoné T, Van Schoubroeck B, Mostmans W, Wuyts D, Verstappen D, Scholliers A, De Pooter D, Dhuyvetter D, Borghys H, Tuefferd M, Arnoult E, Hong J, Fanning G, Bollekens J, Urmaliya V, Teisman A, Horton H, Jonckers THM, Raboisson P. McGowan DC, et al. Among authors: last s. J Med Chem. 2017 Jul 27;60(14):6137-6151. doi: 10.1021/acs.jmedchem.7b00365. Epub 2017 Jul 14. J Med Chem. 2017. PMID: 28671847
Characterization of a dengue NS4B inhibitor originating from an HCV small molecule library.
Hernandez-Morales I, Geluykens P, Clynhens M, Strijbos R, Goethals O, Megens S, Verheyen N, Last S, McGowan D, Coesemans E, De Boeck B, Stoops B, Devogelaere B, Pauwels F, Vandyck K, Berke JM, Raboisson P, Simmen K, Lory P, Van Loock M. Hernandez-Morales I, et al. Among authors: last s. Antiviral Res. 2017 Nov;147:149-158. doi: 10.1016/j.antiviral.2017.10.011. Epub 2017 Oct 14. Antiviral Res. 2017. PMID: 29037976
24 results