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Page 1
Discovery of the First Potent and Selective Inhibitor of Centromere-Associated Protein E: GSK923295.
Qian X, McDonald A, Zhou HJ, Adams ND, Parrish CA, Duffy KJ, Fitch DM, Tedesco R, Ashcraft LW, Yao B, Jiang H, Huang JK, Marin MV, Aroyan CE, Wang J, Ahmed S, Burgess JL, Chaudhari AM, Donatelli CA, Darcy MG, Ridgers LH, Newlander KA, Schmidt SJ, Chai D, Colón M, Zimmerman MN, Lad L, Sakowicz R, Schauer S, Belmont L, Baliga R, Pierce DW, Finer JT, Wang Z, Morgan BP, Morgans DJ Jr, Auger KR, Sung CM, Carson JD, Luo L, Hugger ED, Copeland RA, Sutton D, Elliott JD, Jackson JR, Wood KW, Dhanak D, Bergnes G, Knight SD. Qian X, et al. Among authors: fitch dm. ACS Med Chem Lett. 2010 Jan 19;1(1):30-4. doi: 10.1021/ml900018m. eCollection 2010 Apr 8. ACS Med Chem Lett. 2010. PMID: 24900171 Free PMC article.
3-(1,1-dioxo-2H-(1,2,4)-benzothiadiazin-3-yl)-4-hydroxy-2(1H)-quinolinones, potent inhibitors of hepatitis C virus RNA-dependent RNA polymerase.
Tedesco R, Shaw AN, Bambal R, Chai D, Concha NO, Darcy MG, Dhanak D, Fitch DM, Gates A, Gerhardt WG, Halegoua DL, Han C, Hofmann GA, Johnston VK, Kaura AC, Liu N, Keenan RM, Lin-Goerke J, Sarisky RT, Wiggall KJ, Zimmerman MN, Duffy KJ. Tedesco R, et al. Among authors: fitch dm. J Med Chem. 2006 Feb 9;49(3):971-83. doi: 10.1021/jm050855s. J Med Chem. 2006. PMID: 16451063
Synthesis and biological activity of heteroaryl 3-(1,1-dioxo-2H-(1,2,4)-benzothiadizin-3-yl)-4-hydroxy-2(1H)-quinolinone derivatives as hepatitis C virus NS5B polymerase inhibitors.
Tedesco R, Chai D, Darcy MG, Dhanak D, Fitch DM, Gates A, Johnston VK, Keenan RM, Lin-Goerke J, Sarisky RT, Shaw AN, Valko KL, Wiggall KJ, Zimmerman MN, Duffy KJ. Tedesco R, et al. Among authors: fitch dm. Bioorg Med Chem Lett. 2009 Aug 1;19(15):4354-8. doi: 10.1016/j.bmcl.2009.05.080. Epub 2009 May 27. Bioorg Med Chem Lett. 2009. PMID: 19505821
Substituted benzothiadizine inhibitors of Hepatitis C virus polymerase.
Shaw AN, Tedesco R, Bambal R, Chai D, Concha NO, Darcy MG, Dhanak D, Duffy KJ, Fitch DM, Gates A, Johnston VK, Keenan RM, Lin-Goerke J, Liu N, Sarisky RT, Wiggall KJ, Zimmerman MN. Shaw AN, et al. Among authors: fitch dm. Bioorg Med Chem Lett. 2009 Aug 1;19(15):4350-3. doi: 10.1016/j.bmcl.2009.05.091. Epub 2009 May 28. Bioorg Med Chem Lett. 2009. PMID: 19515564
Discovery and Preclinical Characterization of GSK1278863 (Daprodustat), a Small Molecule Hypoxia Inducible Factor-Prolyl Hydroxylase Inhibitor for Anemia.
Ariazi JL, Duffy KJ, Adams DF, Fitch DM, Luo L, Pappalardi M, Biju M, DiFilippo EH, Shaw T, Wiggall K, Erickson-Miller C. Ariazi JL, et al. Among authors: fitch dm. J Pharmacol Exp Ther. 2017 Dec;363(3):336-347. doi: 10.1124/jpet.117.242503. Epub 2017 Sep 19. J Pharmacol Exp Ther. 2017. PMID: 28928122
Asymmetric Synthesis of Phorboxazole B-Part II: Synthesis of the C(1)-C(19) Subunit and Fragment Assembly Financial support has been provided by the National Institutes of Health (GM-33328) and the National Science Foundation. The NIH BRS Shared Instrumentation Grant Program 1-S10-RR04870 and the NSF (CHE 88-14019) are acknowledged for providing NMR facilities.
Evans DA, Fitch DM. Evans DA, et al. Among authors: fitch dm. Angew Chem Int Ed Engl. 2000 Jul 17;39(14):2536-2540. doi: 10.1002/1521-3773(20000717)39:14<2536::aid-anie2536>3.0.co;2-u. Angew Chem Int Ed Engl. 2000. PMID: 10941128 No abstract available.
Asymmetric Synthesis of Phorboxazole B-Part I: Synthesis of the C(20)-C(38) and C(39)-C(46) Subunits Financial support was provided by the National Institutes of Health (GM-33328) and the National Science Foundation. An American Cancer Society Postdoctoral Fellowship to T.E.S. and an NSF Predoctoral Fellowship to V.J.C. are gratefully acknowledged. The NIH BRS Shared Instrumentation Grant Program 1-S10-RR04870 and the NSF (CHE 88-14019) are acknowledged for providing NMR facilities.
Evans DA, Cee VJ, Smith TE, Fitch DM, Cho PS. Evans DA, et al. Among authors: fitch dm. Angew Chem Int Ed Engl. 2000 Jul 17;39(14):2533-2536. doi: 10.1002/1521-3773(20000717)39:14<2533::aid-anie2533>3.0.co;2-b. Angew Chem Int Ed Engl. 2000. PMID: 10941127 No abstract available.
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