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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. 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: cowan dj. 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
Discovery of a highly potent, nonabsorbable apical sodium-dependent bile acid transporter inhibitor (GSK2330672) for treatment of type 2 diabetes.
Wu Y, Aquino CJ, Cowan DJ, Anderson DL, Ambroso JL, Bishop MJ, Boros EE, Chen L, Cunningham A, Dobbins RL, Feldman PL, Harston LT, Kaldor IW, Klein R, Liang X, McIntyre MS, Merrill CL, Patterson KM, Prescott JS, Ray JS, Roller SG, Yao X, Young A, Yuen J, Collins JL. Wu Y, et al. Among authors: cowan dj. J Med Chem. 2013 Jun 27;56(12):5094-114. doi: 10.1021/jm400459m. Epub 2013 Jun 6. J Med Chem. 2013. PMID: 23678871
Substrate specificity and novel selective inhibitors of TNF-alpha converting enzyme (TACE) from two-dimensional substrate mapping.
Lambert MH, Blackburn RK, Seaton TD, Kassel DB, Kinder DS, Leesnitzer MA, Bickett DM, Warner JR, Andersen MW, Badiang JG, Cowan DJ, Gaul MD, Petrov KG, Rabinowitz MH, Wiethe RW, Becherer JD, McDougald DL, Musso DL, Andrews RC, Moss ML. Lambert MH, et al. Among authors: cowan dj. Comb Chem High Throughput Screen. 2005 Jun;8(4):327-39. doi: 10.2174/1386207054020840. Comb Chem High Throughput Screen. 2005. PMID: 16101009
N-hydroxyformamide peptidomimetics as TACE/matrix metalloprotease inhibitors: oral activity via P1' isobutyl substitution.
Musso DL, Andersen MW, Andrews RC, Austin R, Beaudet EJ, Becherer JD, Bubacz DG, Bickett DM, Chan JH, Conway JG, Cowan DJ, Gaul MD, Glennon KC, Hedeen KM, Lambert MH, Leesnitzer MA, McDougald DL, Mitchell JL, Moss ML, Rabinowitz MH, Rizzolio MC, Schaller LT, Stanford JB, Tippin T, Warner JR, Whitesell LG, Wiethe RW. Musso DL, et al. Among authors: cowan dj. Bioorg Med Chem Lett. 2001 Aug 20;11(16):2147-51. doi: 10.1016/s0960-894x(01)00377-8. Bioorg Med Chem Lett. 2001. PMID: 11514157
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