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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: haffner cd. 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
Genetic Ablation of CD38 Protects against Western Diet-Induced Exercise Intolerance and Metabolic Inflexibility.
Chiang SH, Harrington WW, Luo G, Milliken NO, Ulrich JC, Chen J, Rajpal DK, Qian Y, Carpenter T, Murray R, Geske RS, Stimpson SA, Kramer HF, Haffner CD, Becherer JD, Preugschat F, Billin AN. Chiang SH, et al. Among authors: haffner cd. PLoS One. 2015 Aug 19;10(8):e0134927. doi: 10.1371/journal.pone.0134927. eCollection 2015. PLoS One. 2015. PMID: 26287487 Free PMC article.
Structure-activity relationships for inhibition of type 1 and 2 human 5 alpha-reductase and human adrenal 3 beta-hydroxy-delta 5-steroid dehydrogenase/3-keto-delta 5-steroid isomerase by 6-azaandrost-4-en-3-ones: optimization of the C17 substituent.
Frye SV, Haffner CD, Maloney PR, Hiner RN, Dorsey GF, Noe RA, Unwalla RJ, Batchelor KW, Bramson HN, Stuart JD, et al. Frye SV, et al. Among authors: haffner cd. J Med Chem. 1995 Jul 7;38(14):2621-7. doi: 10.1021/jm00014a015. J Med Chem. 1995. PMID: 7629802
2-Cyano-4-fluoro-1-thiovalylpyrrolidine analogues as potent inhibitors of DPP-IV.
Haffner CD, McDougald DL, Reister SM, Thompson BD, Conlee C, Fang J, Bass J, Lenhard JM, Croom D, Secosky-Chang MB, Tomaszek T, McConn D, Wells-Knecht K, Johnson PR. Haffner CD, et al. Bioorg Med Chem Lett. 2005 Dec 1;15(23):5257-61. doi: 10.1016/j.bmcl.2005.08.050. Epub 2005 Sep 15. Bioorg Med Chem Lett. 2005. PMID: 16168640
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