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Page 1
6-Substituted quinolines as RORγt inverse agonists.
Barbay JK, Cummings MD, Abad M, Castro G, Kreutter KD, Kummer DA, Maharoof U, Milligan C, Nishimura R, Pierce J, Schalk-Hihi C, Spurlino J, Tanis VM, Urbanski M, Venkatesan H, Wang A, Woods C, Wolin R, Xue X, Edwards JP, Fourie AM, Leonard K. Barbay JK, et al. Among authors: leonard k. Bioorg Med Chem Lett. 2017 Dec 1;27(23):5277-5283. doi: 10.1016/j.bmcl.2017.10.027. Epub 2017 Oct 16. Bioorg Med Chem Lett. 2017. PMID: 29079472
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 structure activity relationships of quinoline tertiary alcohol modulators of RORγt.
Kummer DA, Cummings MD, Abad M, Barbay J, Castro G, Wolin R, Kreutter KD, Maharoof U, Milligan C, Nishimura R, Pierce J, Schalk-Hihi C, Spurlino J, Urbanski M, Venkatesan H, Wang A, Woods C, Xue X, Edwards JP, Fourie AM, Leonard K. Kummer DA, et al. Among authors: leonard k. Bioorg Med Chem Lett. 2017 May 1;27(9):2047-2057. doi: 10.1016/j.bmcl.2017.02.044. Epub 2017 Feb 21. Bioorg Med Chem Lett. 2017. PMID: 28318945
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: leonard k. 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
3-Substituted Quinolines as RORγt Inverse Agonists.
Tanis VM, Venkatesan H, Cummings MD, Albers M, Kent Barbay J, Herman K, Kummer DA, Milligan C, Nelen MI, Nishimura R, Schlueter T, Scott B, Spurlino J, Wolin R, Woods C, Xue X, Edwards JP, Fourie AM, Leonard K. Tanis VM, et al. Among authors: leonard k. Bioorg Med Chem Lett. 2019 Jun 15;29(12):1463-1470. doi: 10.1016/j.bmcl.2019.04.021. Epub 2019 Apr 12. Bioorg Med Chem Lett. 2019. PMID: 31010722
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: leonard k. 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 of a Gut-Restricted JAK Inhibitor for the Treatment of Inflammatory Bowel Disease.
Leonard KA, Madge LA, Krawczuk PJ, Wang A, Kreutter KD, Bacani GM, Chai W, Smith RC, Tichenor MS, Harris MC, Malaviya R, Seierstad M, Johnson ME, Venable JD, Kim S, Hirst GC, Mathur AS, Rao TS, Edwards JP, Rizzolio MC, Koudriakova T. Leonard KA, et al. J Med Chem. 2020 Mar 26;63(6):2915-2929. doi: 10.1021/acs.jmedchem.9b01439. Epub 2020 Mar 16. J Med Chem. 2020. PMID: 32134643
Discovery of a Potent and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase with Oral Anti-Inflammatory Activity.
Tichenor MS, Wiener JJM, Rao NL, Pooley Deckhut C, Barbay JK, Kreutter KD, Bacani GM, Wei J, Chang L, Murrey HE, Wang W, Ahn K, Huber M, Rex E, Coe KJ, Wu J, Seierstad M, Bembenek SD, Leonard KA, Lebsack AD, Venable JD, Edwards JP. Tichenor MS, et al. Among authors: leonard ka. ACS Med Chem Lett. 2021 Apr 5;12(5):782-790. doi: 10.1021/acsmedchemlett.1c00044. eCollection 2021 May 13. ACS Med Chem Lett. 2021. PMID: 34055226 Free PMC article.
Enantiomerically pure 1,4-benzodiazepine-2,5-diones as Hdm2 antagonists.
Marugan JJ, Leonard K, Raboisson P, Gushue JM, Calvo R, Koblish HK, Lattanze J, Zhao S, Cummings MD, Player MR, Schubert C, Maroney AC, Lu T. Marugan JJ, et al. Among authors: leonard k. Bioorg Med Chem Lett. 2006 Jun 15;16(12):3115-20. doi: 10.1016/j.bmcl.2006.03.067. Epub 2006 Apr 21. Bioorg Med Chem Lett. 2006. PMID: 16630722
Optimization of arylindenopyrimidines as potent adenosine A(2A)/A(1) antagonists.
Shook BC, Rassnick S, Chakravarty D, Wallace N, Ault M, Crooke J, Barbay JK, Wang A, Leonard K, Powell MT, Alford V, Hall D, Rupert KC, Heintzelman GR, Hansen K, Bullington JL, Scannevin RH, Carroll K, Lampron L, Westover L, Russell R, Branum S, Wells K, Damon S, Youells S, Beauchamp D, Li X, Rhodes K, Jackson PF. Shook BC, et al. Among authors: leonard k. Bioorg Med Chem Lett. 2010 May 1;20(9):2868-71. doi: 10.1016/j.bmcl.2010.03.024. Epub 2010 Mar 7. Bioorg Med Chem Lett. 2010. PMID: 20338760
743 results