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19 results

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Page 1
JDQ443, a Structurally Novel, Pyrazole-Based, Covalent Inhibitor of KRASG12C for the Treatment of Solid Tumors.
Lorthiois E, Gerspacher M, Beyer KS, Vaupel A, Leblanc C, Stringer R, Weiss A, Wilcken R, Guthy DA, Lingel A, Bomio-Confaglia C, Machauer R, Rigollier P, Ottl J, Arz D, Bernet P, Desjonqueres G, Dussauge S, Kazic-Legueux M, Lozac'h MA, Mura C, Sorge M, Todorov M, Warin N, Zink F, Voshol H, Zecri FJ, Sedrani RC, Ostermann N, Brachmann SM, Cotesta S. Lorthiois E, et al. Among authors: machauer r. J Med Chem. 2022 Dec 22;65(24):16173-16203. doi: 10.1021/acs.jmedchem.2c01438. Epub 2022 Nov 18. J Med Chem. 2022. PMID: 36399068
Discovery of cyclic sulfone hydroxyethylamines as potent and selective β-site APP-cleaving enzyme 1 (BACE1) inhibitors: structure-based design and in vivo reduction of amyloid β-peptides.
Rueeger H, Lueoend R, Rogel O, Rondeau JM, Möbitz H, Machauer R, Jacobson L, Staufenbiel M, Desrayaud S, Neumann U. Rueeger H, et al. Among authors: machauer r. J Med Chem. 2012 Apr 12;55(7):3364-86. doi: 10.1021/jm300069y. Epub 2012 Mar 21. J Med Chem. 2012. PMID: 22380629
Discovery of cyclic sulfoxide hydroxyethylamines as potent and selective β-site APP-cleaving enzyme 1 (BACE1) inhibitors: structure based design and in vivo reduction of amyloid β-peptides.
Rueeger H, Lueoend R, Machauer R, Veenstra SJ, Jacobson LH, Staufenbiel M, Desrayaud S, Rondeau JM, Möbitz H, Neumann U. Rueeger H, et al. Among authors: machauer r. Bioorg Med Chem Lett. 2013 Oct 1;23(19):5300-6. doi: 10.1016/j.bmcl.2013.07.071. Epub 2013 Aug 9. Bioorg Med Chem Lett. 2013. PMID: 23981898
Discovery of Novel Dot1L Inhibitors through a Structure-Based Fragmentation Approach.
Chen C, Zhu H, Stauffer F, Caravatti G, Vollmer S, Machauer R, Holzer P, Möbitz H, Scheufler C, Klumpp M, Tiedt R, Beyer KS, Calkins K, Guthy D, Kiffe M, Zhang J, Gaul C. Chen C, et al. Among authors: machauer r. ACS Med Chem Lett. 2016 Jun 1;7(8):735-40. doi: 10.1021/acsmedchemlett.6b00167. eCollection 2016 Aug 11. ACS Med Chem Lett. 2016. PMID: 27563395 Free PMC article.
Discovery of Potent, Selective, and Structurally Novel Dot1L Inhibitors by a Fragment Linking Approach.
Möbitz H, Machauer R, Holzer P, Vaupel A, Stauffer F, Ragot C, Caravatti G, Scheufler C, Fernandez C, Hommel U, Tiedt R, Beyer KS, Chen C, Zhu H, Gaul C. Möbitz H, et al. Among authors: machauer r. ACS Med Chem Lett. 2017 Feb 14;8(3):338-343. doi: 10.1021/acsmedchemlett.6b00519. eCollection 2017 Mar 9. ACS Med Chem Lett. 2017. PMID: 28337327 Free PMC article.
Macrocyclic peptidomimetic beta-secretase (BACE-1) inhibitors with activity in vivo.
Machauer R, Laumen K, Veenstra S, Rondeau JM, Tintelnot-Blomley M, Betschart C, Jaton AL, Desrayaud S, Staufenbiel M, Rabe S, Paganetti P, Neumann U. Machauer R, et al. Bioorg Med Chem Lett. 2009 Mar 1;19(5):1366-70. doi: 10.1016/j.bmcl.2009.01.055. Epub 2009 Jan 22. Bioorg Med Chem Lett. 2009. PMID: 19195887
Macrocyclic BACE-1 inhibitors acutely reduce Abeta in brain after po application.
Lerchner A, Machauer R, Betschart C, Veenstra S, Rueeger H, McCarthy C, Tintelnot-Blomley M, Jaton AL, Rabe S, Desrayaud S, Enz A, Staufenbiel M, Paganetti P, Rondeau JM, Neumann U. Lerchner A, et al. Among authors: machauer r. Bioorg Med Chem Lett. 2010 Jan 15;20(2):603-7. doi: 10.1016/j.bmcl.2009.11.092. Epub 2009 Nov 22. Bioorg Med Chem Lett. 2010. PMID: 19963375
Discovery of amino-1,4-oxazines as potent BACE-1 inhibitors.
Veenstra SJ, Rueeger H, Voegtle M, Lueoend R, Holzer P, Hurth K, Tintelnot-Blomley M, Frederiksen M, Rondeau JM, Jacobson L, Staufenbiel M, Neumann U, Machauer R. Veenstra SJ, et al. Among authors: machauer r. Bioorg Med Chem Lett. 2018 Jul 1;28(12):2195-2200. doi: 10.1016/j.bmcl.2018.05.003. Epub 2018 May 3. Bioorg Med Chem Lett. 2018. PMID: 29764741
19 results