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Items: 12

1.

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.

J Pharmacol Exp Ther. 2017 Dec;363(3):336-347. doi: 10.1124/jpet.117.242503. Epub 2017 Sep 19.

2.

New IDH1 mutant inhibitors for treatment of acute myeloid leukemia.

Okoye-Okafor UC, Bartholdy B, Cartier J, Gao EN, Pietrak B, Rendina AR, Rominger C, Quinn C, Smallwood A, Wiggall KJ, Reif AJ, Schmidt SJ, Qi H, Zhao H, Joberty G, Faelth-Savitski M, Bantscheff M, Drewes G, Duraiswami C, Brady P, Groy A, Narayanagari SR, Antony-Debre I, Mitchell K, Wang HR, Kao YR, Christopeit M, Carvajal L, Barreyro L, Paietta E, Makishima H, Will B, Concha N, Adams ND, Schwartz B, McCabe MT, Maciejewski J, Verma A, Steidl U.

Nat Chem Biol. 2015 Nov;11(11):878-86. doi: 10.1038/nchembio.1930. Epub 2015 Oct 5.

3.

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.

Bioorg Med Chem Lett. 2009 Aug 1;19(15):4350-3. doi: 10.1016/j.bmcl.2009.05.091. Epub 2009 May 28.

PMID:
19515564
4.

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.

Bioorg Med Chem Lett. 2009 Aug 1;19(15):4354-8. doi: 10.1016/j.bmcl.2009.05.080. Epub 2009 May 27.

PMID:
19505821
5.

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.

J Med Chem. 2006 Feb 9;49(3):971-83.

PMID:
16451063
6.

Identification of a pharmacophore for thrombopoietic activity of small, non-peptidyl molecules. 2. Rational design of naphtho[1,2-d]imidazole thrombopoietin mimics.

Duffy KJ, Price AT, Delorme E, Dillon SB, Duquenne C, Erickson-Miller C, Giampa L, Huang Y, Keenan RM, Lamb P, Liu N, Miller SG, Rosen J, Shaw AN, Smith H, Wiggall KJ, Zhang L, Luengo JI.

J Med Chem. 2002 Aug 15;45(17):3576-8.

PMID:
12166929
7.

Identification of a pharmacophore for thrombopoietic activity of small, non-peptidyl molecules. 1. Discovery and optimization of salicylaldehyde thiosemicarbazone thrombopoietin mimics.

Duffy KJ, Shaw AN, Delorme E, Dillon SB, Erickson-Miller C, Giampa L, Huang Y, Keenan RM, Lamb P, Liu N, Miller SG, Price AT, Rosen J, Smith H, Wiggall KJ, Zhang L, Luengo JI.

J Med Chem. 2002 Aug 15;45(17):3573-5.

PMID:
12166928
8.

Hydrazinonaphthalene and azonaphthalene thrombopoietin mimics are nonpeptidyl promoters of megakaryocytopoiesis.

Duffy KJ, Darcy MG, Delorme E, Dillon SB, Eppley DF, Erickson-Miller C, Giampa L, Hopson CB, Huang Y, Keenan RM, Lamb P, Leong L, Liu N, Miller SG, Price AT, Rosen J, Shah R, Shaw TN, Smith H, Stark KC, Tian SS, Tyree C, Wiggall KJ, Zhang L, Luengo JI.

J Med Chem. 2001 Oct 25;44(22):3730-45.

PMID:
11606138
9.

Reversible inhibitors of the gastric (H+/K+)-ATPase. 4. Identification of an inhibitor with an intermediate duration of action.

Leach CA, Brown TH, Ife RJ, Keeling DJ, Parsons ME, Theobald CJ, Wiggall KJ.

J Med Chem. 1995 Jul 7;38(14):2748-62.

PMID:
7629813
10.

Reversible inhibitors of the gastric (H+/K+)-ATPase. 3. 3-substituted-4-(phenylamino)quinolines.

Ife RJ, Brown TH, Keeling DJ, Leach CA, Meeson ML, Parsons ME, Reavill DR, Theobald CJ, Wiggall KJ.

J Med Chem. 1992 Sep 4;35(18):3413-22.

PMID:
1326634
11.

Reversible inhibitors of the gastric (H+/K+)-ATPase. 2. 1-Arylpyrrolo[3,2-c]quinolines: effect of the 4-substituent.

Leach CA, Brown TH, Ife RJ, Keeling DJ, Laing SM, Parsons ME, Price CA, Wiggall KJ.

J Med Chem. 1992 May 15;35(10):1845-52.

PMID:
1316968
12.

Reversible inhibitors of the gastric (H+/K+)-ATPase. 1. 1-Aryl-4-methylpyrrolo[3,2-c]quinolines as conformationally restrained analogues of 4-(arylamino)quinolines.

Brown TH, Ife RJ, Keeling DJ, Laing SM, Leach CA, Parsons ME, Price CA, Reavill DR, Wiggall KJ.

J Med Chem. 1990 Feb;33(2):527-33.

PMID:
2153816

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