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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: fourie am. 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
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. 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
Azabenzthiazole inhibitors of leukotriene A₄ hydrolase.
Tanis VM, Bacani GM, Blevitt JM, Chrovian CC, Crawford S, De Leon A, Fourie AM, Gomez L, Grice CA, Herman K, Kearney AM, Landry-Bayle AM, Lee-Dutra A, Nelson J, Riley JP, Santillán A Jr, Wiener JJ, Xue X, Young AL. Tanis VM, et al. Among authors: fourie am. Bioorg Med Chem Lett. 2012 Dec 15;22(24):7504-11. doi: 10.1016/j.bmcl.2012.10.036. Epub 2012 Oct 17. Bioorg Med Chem Lett. 2012. PMID: 23127888
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: fourie am. 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
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: fourie am. 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. Among authors: fourie am. 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: fourie am. 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
RORγt and RORα signature genes in human Th17 cells.
Castro G, Liu X, Ngo K, De Leon-Tabaldo A, Zhao S, Luna-Roman R, Yu J, Cao T, Kuhn R, Wilkinson P, Herman K, Nelen MI, Blevitt J, Xue X, Fourie A, Fung-Leung WP. Castro G, et al. PLoS One. 2017 Aug 1;12(8):e0181868. doi: 10.1371/journal.pone.0181868. eCollection 2017. PLoS One. 2017. PMID: 28763457 Free PMC article.
Identification of benzofuran central cores for the inhibition of leukotriene A(4) hydrolase.
Eccles W, Blevitt JM, Booker JN, Chrovian CC, Crawford S, de Leon AR, Deng X, Fourie AM, Grice CA, Herman K, Karlsson L, Kearney AM, Lee-Dutra A, Liang J, Luna R, Pippel D, Rao N, Riley JP, Santillán A, Savall B, Tanis VM, Xue X, Young AL. Eccles W, et al. Among authors: fourie am. Bioorg Med Chem Lett. 2013 Feb 1;23(3):811-5. doi: 10.1016/j.bmcl.2012.11.074. Epub 2012 Dec 5. Bioorg Med Chem Lett. 2013. PMID: 23260350
44 results