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Page 1
Design of HIV-1 protease inhibitors active on multidrug-resistant virus.
Surleraux DL, de Kock HA, Verschueren WG, Pille GM, Maes LJ, Peeters A, Vendeville S, De Meyer S, Azijn H, Pauwels R, de Bethune MP, King NM, Prabu-Jeyabalan M, Schiffer CA, Wigerinck PB. Surleraux DL, et al. Among authors: de kock ha, de bethune mp, de meyer s. J Med Chem. 2005 Mar 24;48(6):1965-73. doi: 10.1021/jm049454n. J Med Chem. 2005. PMID: 15771440
Discovery and selection of TMC114, a next generation HIV-1 protease inhibitor.
Surleraux DL, Tahri A, Verschueren WG, Pille GM, de Kock HA, Jonckers TH, Peeters A, De Meyer S, Azijn H, Pauwels R, de Bethune MP, King NM, Prabu-Jeyabalan M, Schiffer CA, Wigerinck PB. Surleraux DL, et al. Among authors: de kock ha, de bethune mp, de meyer s. J Med Chem. 2005 Mar 24;48(6):1813-22. doi: 10.1021/jm049560p. J Med Chem. 2005. PMID: 15771427
Rapid HCV-RNA decline with once daily TMC435: a phase I study in healthy volunteers and hepatitis C patients.
Reesink HW, Fanning GC, Farha KA, Weegink C, Van Vliet A, Van 't Klooster G, Lenz O, Aharchi F, Mariën K, Van Remoortere P, de Kock H, Broeckaert F, Meyvisch P, Van Beirendonck E, Simmen K, Verloes R. Reesink HW, et al. Among authors: de kock h. Gastroenterology. 2010 Mar;138(3):913-21. doi: 10.1053/j.gastro.2009.10.033. Epub 2009 Oct 21. Gastroenterology. 2010. PMID: 19852962 Clinical Trial.
Structure-activity relationship study on a novel series of cyclopentane-containing macrocyclic inhibitors of the hepatitis C virus NS3/4A protease leading to the discovery of TMC435350.
Raboisson P, de Kock H, Rosenquist A, Nilsson M, Salvador-Oden L, Lin TI, Roue N, Ivanov V, Wähling H, Wickström K, Hamelink E, Edlund M, Vrang L, Vendeville S, Van de Vreken W, McGowan D, Tahri A, Hu L, Boutton C, Lenz O, Delouvroy F, Pille G, Surleraux D, Wigerinck P, Samuelsson B, Simmen K. Raboisson P, et al. Among authors: de kock h. Bioorg Med Chem Lett. 2008 Sep 1;18(17):4853-8. doi: 10.1016/j.bmcl.2008.07.088. Epub 2008 Jul 24. Bioorg Med Chem Lett. 2008. PMID: 18678486
Discovery of novel, potent and bioavailable proline-urea based macrocyclic HCV NS3/4A protease inhibitors.
Vendeville S, Nilsson M, de Kock H, Lin TI, Antonov D, Classon B, Ayesa S, Ivanov V, Johansson PO, Kahnberg P, Eneroth A, Wikstrom K, Vrang L, Edlund M, Lindström S, Van de Vreken W, McGowan D, Tahri A, Hu L, Lenz O, Delouvroy F, Van Dooren M, Kindermans N, Surleraux D, Wigerinck P, Rosenquist A, Samuelsson B, Simmen K, Raboisson P. Vendeville S, et al. Among authors: de kock h. Bioorg Med Chem Lett. 2008 Dec 1;18(23):6189-93. doi: 10.1016/j.bmcl.2008.10.004. Epub 2008 Oct 5. Bioorg Med Chem Lett. 2008. PMID: 18954982
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: de kock h. J Med Chem. 2010 Nov 25;53(22):8150-60. doi: 10.1021/jm101050a. Epub 2010 Oct 29. J Med Chem. 2010. PMID: 21033671
In vitro activity and preclinical profile of TMC435350, a potent hepatitis C virus protease inhibitor.
Lin TI, Lenz O, Fanning G, Verbinnen T, Delouvroy F, Scholliers A, Vermeiren K, Rosenquist A, Edlund M, Samuelsson B, Vrang L, de Kock H, Wigerinck P, Raboisson P, Simmen K. Lin TI, et al. Among authors: de kock h. Antimicrob Agents Chemother. 2009 Apr;53(4):1377-85. doi: 10.1128/AAC.01058-08. Epub 2009 Jan 26. Antimicrob Agents Chemother. 2009. PMID: 19171797 Free PMC article.
Synthesis and SAR of potent inhibitors of the Hepatitis C virus NS3/4A protease: exploration of P2 quinazoline substituents.
Nilsson M, Belfrage AK, Lindström S, Wähling H, Lindquist C, Ayesa S, Kahnberg P, Pelcman M, Benkestock K, Agback T, Vrang L, Terelius Y, Wikström K, Hamelink E, Rydergård C, Edlund M, Eneroth A, Raboisson P, Lin TI, de Kock H, Wigerinck P, Simmen K, Samuelsson B, Rosenquist S. Nilsson M, et al. Among authors: de kock h. Bioorg Med Chem Lett. 2010 Jul 15;20(14):4004-11. doi: 10.1016/j.bmcl.2010.05.029. Epub 2010 May 21. Bioorg Med Chem Lett. 2010. PMID: 20541405
52 results