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Items: 36

1.

Lead optimization toward proof-of-concept tools for Huntington's disease within a 4-(1H-pyrazol-4-yl)pyrimidine class of pan-JNK inhibitors.

Wityak J, McGee KF, Conlon MP, Song RH, Duffy BC, Clayton B, Lynch M, Wang G, Freeman E, Haber J, Kitchen DB, Manning DD, Ismail J, Khmelnitsky Y, Michels P, Webster J, Irigoyen M, Luche M, Hultman M, Bai M, Kuok ID, Newell R, Lamers M, Leonard P, Yates D, Matthews K, Ongeri L, Clifton S, Mead T, Deupree S, Wheelan P, Lyons K, Wilson C, Kiselyov A, Toledo-Sherman L, Beconi M, Muñoz-Sanjuan I, Bard J, Dominguez C.

J Med Chem. 2015 Apr 9;58(7):2967-87. doi: 10.1021/jm5013598. Epub 2015 Mar 19.

PMID:
25760409
2.

Development of a series of aryl pyrimidine kynurenine monooxygenase inhibitors as potential therapeutic agents for the treatment of Huntington's disease.

Toledo-Sherman LM, Prime ME, Mrzljak L, Beconi MG, Beresford A, Brookfield FA, Brown CJ, Cardaun I, Courtney SM, Dijkman U, Hamelin-Flegg E, Johnson PD, Kempf V, Lyons K, Matthews K, Mitchell WL, O'Connell C, Pena P, Powell K, Rassoulpour A, Reed L, Reindl W, Selvaratnam S, Friley WW, Weddell DA, Went NE, Wheelan P, Winkler C, Winkler D, Wityak J, Yarnold CJ, Yates D, Munoz-Sanjuan I, Dominguez C.

J Med Chem. 2015 Feb 12;58(3):1159-83. doi: 10.1021/jm501350y. Epub 2015 Jan 23.

PMID:
25590515
3.

Discovery of a novel series of cyclic urea as potent CCR5 antagonists.

Duan M, Kazmierski WM, Tallant M, Jun JH, Edelstein M, Ferris R, Todd D, Wheelan P, Xiong Z.

Bioorg Med Chem Lett. 2011 Nov 1;21(21):6381-5. doi: 10.1016/j.bmcl.2011.08.096. Epub 2011 Aug 28.

PMID:
21930378
4.

Discovery of novel pyridyl carboxamides as potent CCR5 antagonists and optimization of their pharmacokinetic profile in rats.

Duan M, Kazmierski WM, Chong PY, Deanda F, Edelstein M, Ferris R, Peckham J, Wheelan P, Xiong Z, Zhang H, Nishizawa R, Takaoka Y.

Bioorg Med Chem Lett. 2011 Nov 1;21(21):6470-5. doi: 10.1016/j.bmcl.2011.08.080. Epub 2011 Aug 23.

PMID:
21920742
5.

Novel 4,4-disubstituted piperidine-based C-C chemokine receptor-5 inhibitors with high potency against human immunodeficiency virus-1 and an improved human ether-a-go-go related gene (hERG) profile.

Kazmierski WM, Anderson DL, Aquino C, Chauder BA, Duan M, Ferris R, Kenakin T, Koble CS, Lang DG, McIntyre MS, Peckham J, Watson C, Wheelan P, Spaltenstein A, Wire MB, Svolto A, Youngman M.

J Med Chem. 2011 Jun 9;54(11):3756-67. doi: 10.1021/jm200279v. Epub 2011 May 17.

PMID:
21539377
6.

Synthesis and evaluation of 2-phenyl-1,4-butanediamine-based CCR5 antagonists for the treatment of HIV-1.

Tallant MD, Duan M, Freeman GA, Ferris RG, Edelstein MP, Kazmierski WM, Wheelan PJ.

Bioorg Med Chem Lett. 2011 Mar 1;21(5):1394-8. doi: 10.1016/j.bmcl.2011.01.030. Epub 2011 Jan 11.

PMID:
21292480
7.

Discovery of N-benzyl-N'-(4-pipyridinyl)urea CCR5 antagonists as anti-HIV-1 agents (II): modification of the acyl portion.

Duan M, Peckham J, Edelstein M, Ferris R, Kazmierski WM, Spaltenstein A, Wheelan P, Xiong Z.

Bioorg Med Chem Lett. 2010 Dec 15;20(24):7401-4. doi: 10.1016/j.bmcl.2010.10.042. Epub 2010 Oct 21.

PMID:
21055933
8.

Discovery of N-benzyl-N'-(4-pipyridinyl)urea CCR5 antagonists as anti-HIV-1 agents (I): optimization of the amine portion.

Duan M, Peckham J, Edelstein M, Ferris R, Kazmierski WM, Spaltenstein A, Wheelan P, Xiong Z.

Bioorg Med Chem Lett. 2010 Dec 15;20(24):7397-400. doi: 10.1016/j.bmcl.2010.10.033. Epub 2010 Oct 12.

PMID:
21035337
9.

Synthesis and SAR of novel isoquinoline CXCR4 antagonists with potent anti-HIV activity.

Miller JF, Gudmundsson KS, D'Aurora Richardson L, Jenkinson S, Spaltenstein A, Thomson M, Wheelan P.

Bioorg Med Chem Lett. 2010 May 15;20(10):3026-30.

PMID:
20443225
10.

Novel N-substituted benzimidazole CXCR4 antagonists as potential anti-HIV agents.

Miller JF, Turner EM, Gudmundsson KS, Jenkinson S, Spaltenstein A, Thomson M, Wheelan P.

Bioorg Med Chem Lett. 2010 Apr 1;20(7):2125-8. doi: 10.1016/j.bmcl.2010.02.053. Epub 2010 Feb 14.

PMID:
20207537
11.

Synthesis of a novel tricyclic 1,2,3,4,4a,5,6,10b-octahydro-1,10-phenanthroline ring system and CXCR4 antagonists with potent activity against HIV-1.

Catalano JG, Gudmundsson KS, Svolto A, Boggs SD, Miller JF, Spaltenstein A, Thomson M, Wheelan P, Minick DJ, Phelps DP, Jenkinson S.

Bioorg Med Chem Lett. 2010 Apr 1;20(7):2186-90. doi: 10.1016/j.bmcl.2010.02.030. Epub 2010 Feb 12.

PMID:
20194023
12.

Blockade of X4-tropic HIV-1 cellular entry by GSK812397, a potent noncompetitive CXCR4 receptor antagonist.

Jenkinson S, Thomson M, McCoy D, Edelstein M, Danehower S, Lawrence W, Wheelan P, Spaltenstein A, Gudmundsson K.

Antimicrob Agents Chemother. 2010 Feb;54(2):817-24. doi: 10.1128/AAC.01293-09. Epub 2009 Nov 30.

13.

Imidazopyridine-5,6,7,8-tetrahydro-8-quinolinamine derivatives with potent activity against HIV-1.

Gudmundsson KS, Boggs SD, Catalano JG, Svolto A, Spaltenstein A, Thomson M, Wheelan P, Jenkinson S.

Bioorg Med Chem Lett. 2009 Nov 15;19(22):6399-403. doi: 10.1016/j.bmcl.2009.09.056. Epub 2009 Sep 19.

PMID:
19818609
14.

[2-(4-Phenyl-4-piperidinyl)ethyl]amine based CCR5 antagonists: derivatizations at the N-terminal of the piperidine ring.

Duan M, Aquino C, Ferris R, Kazmierski WM, Kenakin T, Koble C, Wheelan P, Watson C, Youngman M.

Bioorg Med Chem Lett. 2009 Mar 15;19(6):1610-3. doi: 10.1016/j.bmcl.2009.02.014. Epub 2009 Feb 10.

PMID:
19233649
15.

Discovery of bioavailable 4,4-disubstituted piperidines as potent ligands of the chemokine receptor 5 and inhibitors of the human immunodeficiency virus-1.

Kazmierski WM, Aquino C, Chauder BA, Deanda F, Ferris R, Jones-Hertzog DK, Kenakin T, Koble CS, Watson C, Wheelan P, Yang H, Youngman M.

J Med Chem. 2008 Oct 23;51(20):6538-46. doi: 10.1021/jm800598a. Epub 2008 Sep 24.

PMID:
18811134
16.

Predicting QT prolongation in humans during early drug development using hERG inhibition and an anaesthetized guinea-pig model.

Yao X, Anderson DL, Ross SA, Lang DG, Desai BZ, Cooper DC, Wheelan P, McIntyre MS, Bergquist ML, MacKenzie KI, Becherer JD, Hashim MA.

Br J Pharmacol. 2008 Aug;154(7):1446-56. doi: 10.1038/bjp.2008.267. Epub 2008 Jun 30.

17.

Synthesis and antiviral activities of novel N-alkoxy-arylsulfonamide-based HIV protease inhibitors.

Sherrill RG, Furfine ES, Hazen RJ, Miller JF, Reynolds DJ, Sammond DM, Spaltenstein A, Wheelan P, Wright LL.

Bioorg Med Chem Lett. 2005 Aug 1;15(15):3560-4.

PMID:
15975788
18.

Metabolic transformations of leukotriene B4 in primary cultures of human hepatocytes.

Wheelan P, Hankin JA, Bilir B, Guenette D, Murphy RC.

J Pharmacol Exp Ther. 1999 Jan;288(1):326-34.

PMID:
9862787
19.
20.

Oxidative metabolism of a rexinoid and rapid phase II metabolite identification by mass spectrometry.

Shirley MA, Wheelan P, Howell SR, Murphy RC.

Drug Metab Dispos. 1997 Oct;25(10):1144-9.

PMID:
9321517
21.

Identification of novel metabolites of prostaglandin E2 formed by isolated rat hepatocytes.

Hankin JA, Wheelan P, Murphy RC.

Arch Biochem Biophys. 1997 Apr 15;340(2):317-30.

PMID:
9143337
23.
24.

Electrospray ionization and low energy tandem mass spectrometry of polyhydroxy unsaturated fatty acids.

Wheelan P, Zirrolli JA, Murphy RC.

J Am Soc Mass Spectrom. 1996 Feb;7(2):140-9. doi: 10.1016/1044-0305(95)00628-1.

PMID:
24203234
25.

Negative ion electrospray tandem mass spectrometric structural characterization of leukotriene B4 (LTB 4) and LTB 4-derived metabolites.

Wheelan P, Zirrolli JA, Murphy RC.

J Am Soc Mass Spectrom. 1996 Feb;7(2):129-39. doi: 10.1016/1044-0305(95)00629-X.

PMID:
24203233
27.

Metabolism of leukotriene B4 in cultured hepatoma cells.

Wheelan P, Murphy RC.

Arch Biochem Biophys. 1995 Aug 20;321(2):381-9.

PMID:
7646063
28.

Analysis of hydroxy fatty acids as pentafluorobenzyl ester, trimethylsilyl ether derivatives by electron ionization gas chromatography/mass spectrometry.

Wheelan P, Zirrolli JA, Murphy RC.

J Am Soc Mass Spectrom. 1995 Jan;6(1):40-51. doi: 10.1016/1044-0305(94)00090-M.

PMID:
24222059
29.

Stereochemical analysis and biological activity of 3-hydroxy-leukotriene B4: a metabolite from ethanol-treated rat hepatocytes.

Wheelan P, Sala A, Folco G, Nicosia S, Falck JR, Bhatt RK, Murphy RC.

J Pharmacol Exp Ther. 1994 Dec;271(3):1514-9.

PMID:
7996465
30.

Metabolism of leukotriene B4 (LTB4) and 12-hydroxy-5,8,10,14-eicosatetraenoic acid (12-HETE) in human keratinocytes.

Wheelan P, Travers JB, Morelli JG, Murphy RC.

Ann N Y Acad Sci. 1994 Nov 15;744:39-49. No abstract available.

PMID:
7825861
31.

Analysis of long-chain fatty acyl coenzyme a thioesters by negative ion fast-atom bombardment mass spectrometry and tandem mass spectrometry.

Zirrolli JA, Wheelan P, Murphy RC.

J Am Soc Mass Spectrom. 1994 May;5(5):416-24. doi: 10.1016/1044-0305(94)85057-7.

PMID:
24222596
32.

Metabolism of leukotriene B4 by cultured human keratinocytes. Formation of glutathione conjugates and dihydro metabolites.

Wheelan P, Zirrolli JA, Morelli JG, Murphy RC.

J Biol Chem. 1993 Dec 5;268(34):25439-48.

33.

Low-energy fast atom bombardment tandem mass spectrometry of monohydroxy substituted unsaturated fatty acids.

Wheelan P, Zirrolli JA, Murphy RC.

Biol Mass Spectrom. 1993 Aug;22(8):465-73.

PMID:
8357860
35.
36.

Successful abdominal pregnancy.

Wheelan P.

Trop Doct. 1989 Jan;19(1):46-7. No abstract available.

PMID:
2922821

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