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Page 1
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: van emelen k. 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: van emelen k. 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: van emelen k. 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
Synthesis and evaluation of novel HCV replication inhibitors.
McGowan DC, Khamlichi MD, De Groot A, Pauwels F, Delouvroy F, Van Emelen K, Simmen K, Raboisson P. McGowan DC, et al. Among authors: van emelen k. Mol Divers. 2017 May;21(2):475-481. doi: 10.1007/s11030-017-9733-z. Epub 2017 Mar 14. Mol Divers. 2017. PMID: 28293834
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: van emelen k. 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
2'-Deoxy-2'-spirocyclopropylcytidine revisited: a new and selective inhibitor of the hepatitis C virus NS5B polymerase.
Jonckers TH, Lin TI, Buyck C, Lachau-Durand S, Vandyck K, Van Hoof S, Vandekerckhove LA, Hu L, Berke JM, Vijgen L, Dillen LL, Cummings MD, de Kock H, Nilsson M, Sund C, Rydegård C, Samuelsson B, Rosenquist A, Fanning G, Van Emelen K, Simmen K, Raboisson P. Jonckers TH, et al. Among authors: van emelen k. J Med Chem. 2010 Nov 25;53(22):8150-60. doi: 10.1021/jm101050a. Epub 2010 Oct 29. J Med Chem. 2010. PMID: 21033671
Design and synthesis of HIV-1 protease inhibitors for a long-acting injectable drug application.
Kesteleyn B, Amssoms K, Schepens W, Hache G, Verschueren W, Van De Vreken W, Rombauts K, Meurs G, Sterkens P, Stoops B, Baert L, Austin N, Wegner J, Masungi C, Dierynck I, Lundgren S, Jönsson D, Parkes K, Kalayanov G, Wallberg H, Rosenquist A, Samuelsson B, Van Emelen K, Thuring JW. Kesteleyn B, et al. Among authors: van emelen k. Bioorg Med Chem Lett. 2013 Jan 1;23(1):310-7. doi: 10.1016/j.bmcl.2012.10.095. Epub 2012 Nov 1. Bioorg Med Chem Lett. 2013. PMID: 23177258
R306465 is a novel potent inhibitor of class I histone deacetylases with broad-spectrum antitumoral activity against solid and haematological malignancies.
Arts J, Angibaud P, Mariën A, Floren W, Janssens B, King P, van Dun J, Janssen L, Geerts T, Tuman RW, Johnson DL, Andries L, Jung M, Janicot M, van Emelen K. Arts J, et al. Among authors: van dun j, van emelen k. Br J Cancer. 2007 Nov 19;97(10):1344-53. doi: 10.1038/sj.bjc.6604025. Epub 2007 Nov 13. Br J Cancer. 2007. PMID: 18000499 Free PMC article.
Identification of a series of substituted 2-piperazinyl-5-pyrimidylhydroxamic acids as potent histone deacetylase inhibitors.
Angibaud P, Van Emelen K, Decrane L, van Brandt S, Ten Holte P, Pilatte I, Roux B, Poncelet V, Speybrouck D, Queguiner L, Gaurrand S, Mariën A, Floren W, Janssen L, Verdonck M, van Dun J, van Gompel J, Gilissen R, Mackie C, Du Jardin M, Peeters J, Noppe M, Van Hijfte L, Freyne E, Page M, Janicot M, Arts J. Angibaud P, et al. Among authors: van emelen k. Bioorg Med Chem Lett. 2010 Jan 1;20(1):294-8. doi: 10.1016/j.bmcl.2009.10.118. Epub 2009 Oct 30. Bioorg Med Chem Lett. 2010. PMID: 19906529
15 results