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Optimization and biological evaluation of thiazole-bis-amide inverse agonists of RORγt.
Gege C, Albers M, Kinzel O, Kleymann G, Schlüter T, Steeneck C, Hoffmann T, Xue X, Cummings MD, Spurlino J, Milligan C, Fourie AM, Edwards JP, Leonard K, Coe K, Scott B, Pippel D, Goldberg SD. Gege C, et al. Among authors: steeneck c. Bioorg Med Chem Lett. 2020 Jun 15;30(12):127205. doi: 10.1016/j.bmcl.2020.127205. Epub 2020 Apr 21. Bioorg Med Chem Lett. 2020. PMID: 32336498
Discovery and optimization of new oxadiazole substituted thiazole RORγt inverse agonists through a bioisosteric amide replacement approach.
Steeneck C, Gege C, Kinzel O, Albers M, Kleymann G, Schlüter T, Schulz A, Xue X, Cummings MD, Fourie AM, Leonard KA, Scott B, Edwards JP, Hoffmann T, Goldberg SD. Steeneck C, et al. Bioorg Med Chem Lett. 2020 Jun 15;30(12):127174. doi: 10.1016/j.bmcl.2020.127174. Epub 2020 Apr 7. Bioorg Med Chem Lett. 2020. PMID: 32334912
Identification and biological evaluation of thiazole-based inverse agonists of RORγt.
Gege C, Cummings MD, Albers M, Kinzel O, Kleymann G, Schlüter T, Steeneck C, Nelen MI, Milligan C, Spurlino J, Xue X, Leonard K, Edwards JP, Fourie A, Goldberg SD, Hoffmann T. Gege C, et al. Among authors: steeneck c. Bioorg Med Chem Lett. 2018 May 15;28(9):1446-1455. doi: 10.1016/j.bmcl.2018.03.093. Epub 2018 Apr 3. Bioorg Med Chem Lett. 2018. PMID: 29631962
Development of Cilofexor, an intestinally-biased Farnesoid X Receptor agonist, for the treatment of fatty liver disease.
Hollenback D, Hambruch E, Fink G, Birkel M, Schulz A, Hornberger M, Liu K, Staiger KM, Krol HD, Deuschle U, Steeneck C, Kinzel O, Liles JT, Budas G, Watkins WJ, Kremoser C. Hollenback D, et al. Among authors: steeneck c. J Pharmacol Exp Ther. 2024 Feb 26:JPET-AR-2023-001900. doi: 10.1124/jpet.123.001900. Online ahead of print. J Pharmacol Exp Ther. 2024. PMID: 38409114 Free article.
Synthesis and pharmacological validation of a novel series of non-steroidal FXR agonists.
Abel U, Schlüter T, Schulz A, Hambruch E, Steeneck C, Hornberger M, Hoffmann T, Perović-Ottstadt S, Kinzel O, Burnet M, Deuschle U, Kremoser C. Abel U, et al. Among authors: steeneck c. Bioorg Med Chem Lett. 2010 Aug 15;20(16):4911-7. doi: 10.1016/j.bmcl.2010.06.084. Epub 2010 Jun 19. Bioorg Med Chem Lett. 2010. PMID: 20638278
Novel substituted isoxazole FXR agonists with cyclopropyl, hydroxycyclobutyl and hydroxyazetidinyl linkers: Understanding and improving key determinants of pharmacological properties.
Kinzel O, Steeneck C, Schlüter T, Schulz A, Gege C, Hahn U, Hambruch E, Hornberger M, Spalwisz A, Frick K, Perović-Ottstadt S, Deuschle U, Burnet M, Kremoser C. Kinzel O, et al. Among authors: steeneck c. Bioorg Med Chem Lett. 2016 Aug 1;26(15):3746-53. doi: 10.1016/j.bmcl.2016.05.070. Epub 2016 May 24. Bioorg Med Chem Lett. 2016. PMID: 27268696
12 results