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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: kinzel o. 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
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: kinzel o. 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. 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
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. Among authors: kinzel o. 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
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: kinzel o. 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
Preclinical and clinical characterization of the RORγt inhibitor JNJ-61803534.
Xue X, De Leon-Tabaldo A, Luna-Roman R, Castro G, Albers M, Schoetens F, DePrimo S, Devineni D, Wilde T, Goldberg S, Kinzel O, Hoffmann T, Fourie AM, Thurmond RL. Xue X, et al. Among authors: kinzel o. Sci Rep. 2021 May 26;11(1):11066. doi: 10.1038/s41598-021-90497-9. Sci Rep. 2021. PMID: 34040108 Free PMC article. Clinical Trial.
36 results