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Gut-Restricted Selective Cyclooxygenase-2 (COX-2) Inhibitors for Chemoprevention of Colorectal Cancer.
Zhang Z, Ghosh A, Connolly PJ, King P, Wilde T, Wang J, Dong Y, Li X, Liao D, Chen H, Tian G, Suarez J, Bonnette WG, Pande V, Diloreto KA, Shi Y, Patel S, Pietrak B, Szewczuk L, Sensenhauser C, Dallas S, Edwards JP, Bachman KE, Evans DC. Zhang Z, et al. Among authors: edwards jp. J Med Chem. 2021 Aug 12;64(15):11570-11596. doi: 10.1021/acs.jmedchem.1c00890. Epub 2021 Jul 19. J Med Chem. 2021. PMID: 34279934
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: edwards jp. 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: edwards jp. 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 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. Among authors: edwards jp. 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 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: edwards jp. 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
A carboxylic acid isostere screen of the DHODH inhibitor Brequinar.
DeRatt LG, Christine Pietsch E, Tanner A, Shaffer P, Jacoby E, Wang W, Kazmi F, Zhang X, Attar RM, Edwards JP, Kuduk SD. DeRatt LG, et al. Among authors: edwards jp. Bioorg Med Chem Lett. 2020 Nov 15;30(22):127589. doi: 10.1016/j.bmcl.2020.127589. Epub 2020 Sep 29. Bioorg Med Chem Lett. 2020. PMID: 33007394
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: edwards jp. 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.
223 results