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Page 1
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: vrang l. 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.
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: vrang l. 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
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: vrang l. 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.
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: vrang l. 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.
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: vrang l. 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
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: vrang l. 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
Discovery of 4'-azido-2'-deoxy-2'-C-methyl cytidine and prodrugs thereof: a potent inhibitor of Hepatitis C virus replication.
Nilsson M, Kalayanov G, Winqvist A, Pinho P, Sund C, Zhou XX, Wähling H, Belfrage AK, Pelcman M, Agback T, Benckestock K, Wikström K, Boothee M, Lindqvist A, Rydegård C, Jonckers TH, Vandyck K, Raboisson P, Lin TI, Lachau-Durand S, de Kock H, Smith DB, Martin JA, Klumpp K, Simmen K, Vrang L, Terelius Y, Samuelsson B, Rosenquist S, Johansson NG. Nilsson M, et al. Among authors: vrang l. Bioorg Med Chem Lett. 2012 May 1;22(9):3265-8. doi: 10.1016/j.bmcl.2012.03.021. Epub 2012 Mar 16. Bioorg Med Chem Lett. 2012. PMID: 22472694
Design and synthesis of potent and selective BACE-1 inhibitors.
Björklund C, Oscarson S, Benkestock K, Borkakoti N, Jansson K, Lindberg J, Vrang L, Hallberg A, Rosenquist A, Samuelsson B. Björklund C, et al. Among authors: vrang l. J Med Chem. 2010 Feb 25;53(4):1458-64. doi: 10.1021/jm901168f. J Med Chem. 2010. PMID: 20128595
Symmetric fluoro-substituted diol-based HIV protease inhibitors. Ortho-fluorinated and meta-fluorinated P1/P1'-benzyloxy side groups significantly improve the antiviral activity and preserve binding efficacy.
Lindberg J, Pyring D, Löwgren S, Rosenquist A, Zuccarello G, Kvarnström I, Zhang H, Vrang L, Classon B, Hallberg A, Samuelsson B, Unge T. Lindberg J, et al. Among authors: vrang l. Eur J Biochem. 2004 Nov;271(22):4594-602. doi: 10.1111/j.1432-1033.2004.04431.x. Eur J Biochem. 2004. PMID: 15560801 Free article.
64 results