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Page 1
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: lin ti. 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
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: lin ti. 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 selective dipeptide hepatitis C virus NS3/4A serine protease inhibitors.
Raboisson P, Lin TI, Kock Hd, Vendeville S, Vreken WV, McGowan D, Tahri A, Hu L, Lenz O, Delouvroy F, Surleraux D, Wigerinck P, Nilsson M, Rosenquist S, Samuelsson B, Simmen K. Raboisson P, et al. Among authors: lin ti. Bioorg Med Chem Lett. 2008 Sep 15;18(18):5095-100. doi: 10.1016/j.bmcl.2008.07.124. Epub 2008 Aug 3. Bioorg Med Chem Lett. 2008. PMID: 18722116
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. 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.
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: lin ti. 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
Induced-fit binding of the macrocyclic noncovalent inhibitor TMC435 to its HCV NS3/NS4A protease target.
Cummings MD, Lindberg J, Lin TI, de Kock H, Lenz O, Lilja E, Felländer S, Baraznenok V, Nyström S, Nilsson M, Vrang L, Edlund M, Rosenquist A, Samuelsson B, Raboisson P, Simmen K. Cummings MD, et al. Among authors: lin ti. Angew Chem Int Ed Engl. 2010 Feb 22;49(9):1652-5. doi: 10.1002/anie.200906696. Angew Chem Int Ed Engl. 2010. PMID: 20166108 No abstract available.
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: lin ti. 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.
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: lin ti. 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
81 results