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Page 1
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: dehertogh p. 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
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: dehertogh p. 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: dehertogh p. 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
TMC647055, a potent nonnucleoside hepatitis C virus NS5B polymerase inhibitor with cross-genotypic coverage.
Devogelaere B, Berke JM, Vijgen L, Dehertogh P, Fransen E, Cleiren E, van der Helm L, Nyanguile O, Tahri A, Amssoms K, Lenz O, Cummings MD, Clayton RF, Vendeville S, Raboisson P, Simmen KA, Fanning GC, Lin TI. Devogelaere B, et al. Among authors: dehertogh p. Antimicrob Agents Chemother. 2012 Sep;56(9):4676-84. doi: 10.1128/AAC.00245-12. Epub 2012 Jun 18. Antimicrob Agents Chemother. 2012. PMID: 22710121 Free PMC article.
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: dehertogh p. J Med Chem. 2014 Mar 13;57(5):1880-92. doi: 10.1021/jm401396p. Epub 2013 Nov 8. J Med Chem. 2014. PMID: 24144360
1,5-benzodiazepines, a novel class of hepatitis C virus polymerase nonnucleoside inhibitors.
Nyanguile O, Pauwels F, Van den Broeck W, Boutton CW, Quirynen L, Ivens T, van der Helm L, Vandercruyssen G, Mostmans W, Delouvroy F, Dehertogh P, Cummings MD, Bonfanti JF, Simmen KA, Raboisson P. Nyanguile O, et al. Among authors: dehertogh p. Antimicrob Agents Chemother. 2008 Dec;52(12):4420-31. doi: 10.1128/AAC.00669-08. Epub 2008 Oct 13. Antimicrob Agents Chemother. 2008. PMID: 18852280 Free PMC article.
1a/1b subtype profiling of nonnucleoside polymerase inhibitors of hepatitis C virus.
Nyanguile O, Devogelaere B, Vijgen L, Van den Broeck W, Pauwels F, Cummings MD, De Bondt HL, Vos AM, Berke JM, Lenz O, Vandercruyssen G, Vermeiren K, Mostmans W, Dehertogh P, Delouvroy F, Vendeville S, VanDyck K, Dockx K, Cleiren E, Raboisson P, Simmen KA, Fanning GC. Nyanguile O, et al. Among authors: dehertogh p. J Virol. 2010 Mar;84(6):2923-34. doi: 10.1128/JVI.01980-09. Epub 2010 Jan 13. J Virol. 2010. PMID: 20071590 Free PMC article.
In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435.
Lenz O, Verbinnen T, Lin TI, Vijgen L, Cummings MD, Lindberg J, Berke JM, Dehertogh P, Fransen E, Scholliers A, Vermeiren K, Ivens T, Raboisson P, Edlund M, Storm S, Vrang L, de Kock H, Fanning GC, Simmen KA. Lenz O, et al. Among authors: dehertogh p. Antimicrob Agents Chemother. 2010 May;54(5):1878-87. doi: 10.1128/AAC.01452-09. Epub 2010 Feb 22. Antimicrob Agents Chemother. 2010. PMID: 20176898 Free PMC article.
Antiviral activity and mode of action of TMC647078, a novel nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
Berke JM, Vijgen L, Lachau-Durand S, Powdrill MH, Rawe S, Sjuvarsson E, Eriksson S, Götte M, Fransen E, Dehertogh P, Van den Eynde C, Leclercq L, Jonckers TH, Raboisson P, Nilsson M, Samuelsson B, Rosenquist Å, Fanning GC, Lin TI. Berke JM, et al. Among authors: dehertogh p. Antimicrob Agents Chemother. 2011 Aug;55(8):3812-20. doi: 10.1128/AAC.00214-11. Epub 2011 May 16. Antimicrob Agents Chemother. 2011. PMID: 21576430 Free PMC article.
23 results