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Page 1
Discovery, Synthesis, and Biological Evaluation of Thiazoloquin(az)olin(on)es as Potent CD38 Inhibitors.
Haffner CD, Becherer JD, Boros EE, Cadilla R, Carpenter T, Cowan D, Deaton DN, Guo Y, Harrington W, Henke BR, Jeune MR, Kaldor I, Milliken N, Petrov KG, Preugschat F, Schulte C, Shearer BG, Shearer T, Smalley TL Jr, Stewart EL, Stuart JD, Ulrich JC. Haffner CD, et al. Among authors: deaton dn. J Med Chem. 2015 Apr 23;58(8):3548-71. doi: 10.1021/jm502009h. Epub 2015 Apr 10. J Med Chem. 2015. PMID: 25828863
Discovery of 4-Amino-8-quinoline Carboxamides as Novel, Submicromolar Inhibitors of NAD-Hydrolyzing Enzyme CD38.
Becherer JD, Boros EE, Carpenter TY, Cowan DJ, Deaton DN, Haffner CD, Jeune MR, Kaldor IW, Poole JC, Preugschat F, Rheault TR, Schulte CA, Shearer BG, Shearer TW, Shewchuk LM, Smalley TL Jr, Stewart EL, Stuart JD, Ulrich JC. Becherer JD, et al. Among authors: deaton dn. J Med Chem. 2015 Sep 10;58(17):7021-56. doi: 10.1021/acs.jmedchem.5b00992. Epub 2015 Aug 24. J Med Chem. 2015. PMID: 26267483
The discovery of quinoline-3-carboxamides as hematopoietic prostaglandin D synthase (H-PGDS) inhibitors.
Deaton DN, Do Y, Holt J, Jeune MR, Kramer HF, Larkin AL, Orband-Miller LA, Peckham GE, Poole C, Price DJ, Schaller LT, Shen Y, Shewchuk LM, Stewart EL, Stuart JD, Thomson SA, Ward P, Wilson JW, Xu T, Guss JH, Musetti C, Rendina AR, Affleck K, Anders D, Hancock AP, Hobbs H, Hodgson ST, Hutchinson J, Leveridge MV, Nicholls H, Smith IED, Somers DO, Sneddon HF, Uddin S, Cleasby A, Mortenson PN, Richardson C, Saxty G. Deaton DN, et al. Bioorg Med Chem. 2019 Apr 15;27(8):1456-1478. doi: 10.1016/j.bmc.2019.02.017. Epub 2019 Feb 11. Bioorg Med Chem. 2019. PMID: 30858025
The exploration of aza-quinolines as hematopoietic prostaglandin D synthase (H-PGDS) inhibitors with low brain exposure.
Cadilla R, Deaton DN, Do Y, Elkins PA, Ennulat D, Guss JH, Holt J, Jeune MR, King AG, Klapwijk JC, Kramer HF, Kramer NJ, Laffan SB, Masuria PI, McDougal AV, Mortenson PN, Musetti C, Peckham GE, Pietrak BL, Poole C, Price DJ, Rendina AR, Sati G, Saxty G, Shearer BG, Shewchuk LM, Sneddon HF, Stewart EL, Stuart JD, Thomas DN, Thomson SA, Ward P, Wilson JW, Xu T, Youngman MA. Cadilla R, et al. Among authors: deaton dn. Bioorg Med Chem. 2020 Dec 1;28(23):115791. doi: 10.1016/j.bmc.2020.115791. Epub 2020 Oct 3. Bioorg Med Chem. 2020. PMID: 33059303
A knowledge-based, structural-aided discovery of a novel class of 2-phenylimidazo[1,2-a]pyridine-6-carboxamide H-PGDS inhibitors.
Schulte CA, Deaton DN, Diaz E, Do Y, Gampe RT, Guss JH, Hancock AP, Hobbs H, Hodgson ST, Holt J, Jeune MR, Kahler KM, Kramer HF, Le J, Mortenson PN, Musetti C, Nolte RT, Orband-Miller LA, Peckham GE, Petrov KG, Pietrak BL, Poole C, Price DJ, Saxty G, Shillings A, Smalley TL Jr, Somers DO, Stewart EL, Stuart JD, Thomson SA. Schulte CA, et al. Among authors: deaton dn. Bioorg Med Chem Lett. 2021 Sep 1;47:128113. doi: 10.1016/j.bmcl.2021.128113. Epub 2021 May 13. Bioorg Med Chem Lett. 2021. PMID: 33991628
Exploration of the P2-P3 SAR of aldehyde cathepsin K inhibitors.
Boros EE, Deaton DN, Hassell AM, McFadyen RB, Miller AB, Miller LR, Paulick MG, Shewchuk LM, Thompson JB, Willard DH Jr, Wright LL. Boros EE, et al. Among authors: deaton dn. Bioorg Med Chem Lett. 2004 Jul 5;14(13):3425-9. doi: 10.1016/j.bmcl.2004.04.084. Bioorg Med Chem Lett. 2004. PMID: 15177446
Novel heterocyclic scaffolds of GW4064 as farnesoid X receptor agonists.
Smalley TL Jr, Boggs S, Caravella JA, Chen L, Creech KL, Deaton DN, Kaldor I, Parks DJ. Smalley TL Jr, et al. Among authors: deaton dn. Bioorg Med Chem Lett. 2015 Jan 15;25(2):280-4. doi: 10.1016/j.bmcl.2014.11.050. Epub 2014 Nov 26. Bioorg Med Chem Lett. 2015. PMID: 25499883
38 results