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Items: 1 to 50 of 81

1.

Identification of 4-(Aminomethyl)-6-(trifluoromethyl)-2-(phenoxy)pyridine Derivatives as Potent, Selective, and Orally Efficacious Inhibitors of the Copper-Dependent Amine Oxidase, Lysyl Oxidase-Like 2 (LOXL2).

Rowbottom MW, Bain G, Calderon I, Lasof T, Lonergan D, Lai A, Huang F, Darlington J, Prodanovich P, Santini AM, King CD, Goulet L, Shannon KE, Ma GL, Nguyen K, MacKenna DA, Evans JF, Hutchinson JH.

J Med Chem. 2017 May 25;60(10):4403-4423. doi: 10.1021/acs.jmedchem.7b00345. Epub 2017 May 15.

PMID:
28471663
2.

Small Molecule Lysyl Oxidase-like 2 (LOXL2) Inhibitors: The Identification of an Inhibitor Selective for LOXL2 over LOX.

Hutchinson JH, Rowbottom MW, Lonergan D, Darlington J, Prodanovich P, King CD, Evans JF, Bain G.

ACS Med Chem Lett. 2017 Mar 1;8(4):423-427. doi: 10.1021/acsmedchemlett.7b00014. eCollection 2017 Apr 13.

3.

Selective Inhibition of Autotaxin Is Efficacious in Mouse Models of Liver Fibrosis.

Bain G, Shannon KE, Huang F, Darlington J, Goulet L, Prodanovich P, Ma GL, Santini AM, Stein AJ, Lonergan D, King CD, Calderon I, Lai A, Hutchinson JH, Evans JF.

J Pharmacol Exp Ther. 2017 Jan;360(1):1-13. Epub 2016 Oct 17.

PMID:
27754931
4.

Structural Basis for Inhibition of Human Autotaxin by Four Potent Compounds with Distinct Modes of Binding.

Stein AJ, Bain G, Prodanovich P, Santini AM, Darlington J, Stelzer NM, Sidhu RS, Schaub J, Goulet L, Lonergan D, Calderon I, Evans JF, Hutchinson JH.

Mol Pharmacol. 2015 Dec;88(6):982-92. doi: 10.1124/mol.115.100404. Epub 2015 Sep 14.

PMID:
26371182
5.

Pharmacodynamics, pharmacokinetics and safety of GSK2190915, a novel oral anti-inflammatory 5-lipoxygenase-activating protein inhibitor.

Bain G, King CD, Schaab K, Rewolinski M, Norris V, Ambery C, Bentley J, Yamada M, Santini AM, van de Wetering de Rooij J, Stock N, Zunic J, Hutchinson JH, Evans JF.

Br J Clin Pharmacol. 2013 Mar;75(3):779-90. doi: 10.1111/j.1365-2125.2012.04386.x.

6.

Pharmacodynamics, pharmacokinetics, and safety of AM211: a novel and potent antagonist of the prostaglandin D2 receptor type 2.

Bain G, King CD, Brittain J, Hartung JP, Dearmond I, Stearns B, Truong YP, Hutchinson JH, Evans JF, Holme K.

J Clin Pharmacol. 2012 Oct;52(10):1482-93. Epub 2011 Nov 22.

PMID:
22110163
7.

5-Lipoxygenase-activating protein (FLAP) inhibitors. Part 4: development of 3-[3-tert-butylsulfanyl-1-[4-(6-ethoxypyridin-3-yl)benzyl]-5-(5-methylpyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethylpropionic acid (AM803), a potent, oral, once daily FLAP inhibitor.

Stock NS, Bain G, Zunic J, Li Y, Ziff J, Roppe J, Santini A, Darlington J, Prodanovich P, King CD, Baccei C, Lee C, Rong H, Chapman C, Broadhead A, Lorrain D, Correa L, Hutchinson JH, Evans JF, Prasit P.

J Med Chem. 2011 Dec 8;54(23):8013-29. doi: 10.1021/jm2008369. Epub 2011 Nov 7.

PMID:
22059882
8.

DP2 (CRTh2) antagonism reduces ocular inflammation induced by allergen challenge and respiratory syncytial virus.

Stebbins KJ, Broadhead AR, Musiyenko A, Barik S, Scott JM, Truong YP, Stearns BA, Hutchinson JH, Prasit P, Evans JF, Lorrain DS.

Int Arch Allergy Immunol. 2012;157(3):259-68. doi: 10.1159/000328769. Epub 2011 Oct 28.

PMID:
22042170
9.

Discovery and optimization of a biphenylacetic acid series of prostaglandin D2 receptor DP2 antagonists with efficacy in a murine model of allergic rhinitis.

Scott JM, Baccei C, Bain G, Broadhead A, Evans JF, Fagan P, Hutchinson JH, King C, Lorrain DS, Lee C, Prasit P, Prodanovich P, Santini A, Stearns BA.

Bioorg Med Chem Lett. 2011 Nov 1;21(21):6608-12. doi: 10.1016/j.bmcl.2011.01.024. Epub 2011 Jan 11.

PMID:
21958540
10.

Pharmacology of AM211, a potent and selective prostaglandin D2 receptor type 2 antagonist that is active in animal models of allergic inflammation.

Bain G, Lorrain DS, Stebbins KJ, Broadhead AR, Santini AM, Prodanovich P, Darlington J, King CD, Lee C, Baccei C, Stearns B, Troung Y, Hutchinson JH, Prasit P, Evans JF.

J Pharmacol Exp Ther. 2011 Jul;338(1):290-301. doi: 10.1124/jpet.111.180430. Epub 2011 Apr 12.

PMID:
21487069
11.

Sodium [2'-[(cyclopropanecarbonyl-ethyl-amino)-methyl]-4'-(6-ethoxy-pyridin-3-yl)-6-methoxy-biphenyl-3-yl]-acetate (AM432): a potent, selective prostaglandin D2 receptor antagonist.

Stock N, Volkots D, Stebbins K, Broadhead A, Stearns B, Roppe J, Parr T, Baccei C, Bain G, Chapman C, Correa L, Darlington J, King C, Lee C, Lorrain DS, Prodanovich P, Santini A, Evans JF, Hutchinson JH, Prasit P.

Bioorg Med Chem Lett. 2011 Feb 1;21(3):1036-40. doi: 10.1016/j.bmcl.2010.12.016. Epub 2010 Dec 9.

PMID:
21211969
12.

Pharmacokinetic and pharmacodynamic characterization of an oral lysophosphatidic acid type 1 receptor-selective antagonist.

Swaney JS, Chapman C, Correa LD, Stebbins KJ, Broadhead AR, Bain G, Santini AM, Darlington J, King CD, Baccei CS, Lee C, Parr TA, Roppe JR, Seiders TJ, Ziff J, Prasit P, Hutchinson JH, Evans JF, Lorrain DS.

J Pharmacol Exp Ther. 2011 Mar;336(3):693-700. doi: 10.1124/jpet.110.175901. Epub 2010 Dec 15.

PMID:
21159750
13.

A novel, orally active LPA(1) receptor antagonist inhibits lung fibrosis in the mouse bleomycin model.

Swaney JS, Chapman C, Correa LD, Stebbins KJ, Bundey RA, Prodanovich PC, Fagan P, Baccei CS, Santini AM, Hutchinson JH, Seiders TJ, Parr TA, Prasit P, Evans JF, Lorrain DS.

Br J Pharmacol. 2010 Aug;160(7):1699-713. doi: 10.1111/j.1476-5381.2010.00828.x.

14.

5-Lipoxygenase-activating protein inhibitors. Part 3: 3-{3-tert-Butylsulfanyl-1-[4-(5-methoxy-pyrimidin-2-yl)-benzyl]-5-(5-methyl-pyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethyl-propionic acid (AM643)-A potent FLAP inhibitor suitable for topical administration.

Stock N, Baccei C, Bain G, Chapman C, Correa L, Darlington J, King C, Lee C, Lorrain DS, Prodanovich P, Santini A, Schaab K, Evans JF, Hutchinson JH, Prasit P.

Bioorg Med Chem Lett. 2010 Aug 1;20(15):4598-601. doi: 10.1016/j.bmcl.2010.06.011. Epub 2010 Jun 8.

PMID:
20566292
15.

Seeing the future of bioactive lipid drug targets.

Evans JF, Hutchinson JH.

Nat Chem Biol. 2010 Jul;6(7):476-9. doi: 10.1038/nchembio.394. No abstract available.

PMID:
20559310
16.

Pharmacology of AM803, a novel selective five-lipoxygenase-activating protein (FLAP) inhibitor in rodent models of acute inflammation.

Lorrain DS, Bain G, Correa LD, Chapman C, Broadhead AR, Santini AM, Prodanovich PP, Darlington JV, Stock NS, Zunic J, King CD, Lee C, Baccei CS, Stearns B, Roppe J, Hutchinson JH, Prasit P, Evans JF.

Eur J Pharmacol. 2010 Aug 25;640(1-3):211-8. doi: 10.1016/j.ejphar.2010.05.003. Epub 2010 May 21.

PMID:
20519143
17.

Therapeutic efficacy of AM156, a novel prostanoid DP2 receptor antagonist, in murine models of allergic rhinitis and house dust mite-induced pulmonary inflammation.

Stebbins KJ, Broadhead AR, Correa LD, Scott JM, Truong YP, Stearns BA, Hutchinson JH, Prasit P, Evans JF, Lorrain DS.

Eur J Pharmacol. 2010 Jul 25;638(1-3):142-9. doi: 10.1016/j.ejphar.2010.04.031. Epub 2010 May 4.

PMID:
20447387
18.

Leukotriene B4 inhibitors: US2009054466; US2009227603 and US2009253684.

Hutchinson JH.

Expert Opin Ther Pat. 2010 May;20(5):707-14. doi: 10.1517/13543771003657180.

PMID:
20402547
19.

Pharmacodynamics and pharmacokinetics of AM103, a novel inhibitor of 5-lipoxygenase-activating protein (FLAP).

Bain G, King CD, Rewolinski M, Schaab K, Santini AM, Shapiro D, Moran M, van de Wetering de Rooij S, Roffel AF, Schuilenga-Hut P, Milne GL, Lorrain DS, Li Y, Arruda JM, Hutchinson JH, Prasit P, Evans JF.

Clin Pharmacol Ther. 2010 Apr;87(4):437-44. doi: 10.1038/clpt.2009.301. Epub 2010 Feb 24.

PMID:
20182424
20.

Pharmacological blockade of the DP2 receptor inhibits cigarette smoke-induced inflammation, mucus cell metaplasia, and epithelial hyperplasia in the mouse lung.

Stebbins KJ, Broadhead AR, Baccei CS, Scott JM, Truong YP, Coate H, Stock NS, Santini AM, Fagan P, Prodanovich P, Bain G, Stearns BA, King CD, Hutchinson JH, Prasit P, Evans JF, Lorrain DS.

J Pharmacol Exp Ther. 2010 Mar;332(3):764-75. doi: 10.1124/jpet.109.161919. Epub 2009 Dec 8.

PMID:
19996299
21.

5-Lipoxygenase-activating protein inhibitors. Part 2: 3-{5-((S)-1-Acetyl-2,3-dihydro-1H-indol-2-ylmethoxy)-3-tert-butylsulfanyl-1-[4-(5-methoxy-pyrimidin-2-yl)-benzyl]-1H-indol-2-yl}-2,2-dimethyl-propionic acid (AM679)--a potent FLAP inhibitor.

Stock N, Baccei C, Bain G, Broadhead A, Chapman C, Darlington J, King C, Lee C, Li Y, Lorrain DS, Prodanovich P, Rong H, Santini A, Zunic J, Evans JF, Hutchinson JH, Prasit P.

Bioorg Med Chem Lett. 2010 Jan 1;20(1):213-7. doi: 10.1016/j.bmcl.2009.10.131. Epub 2009 Oct 31.

PMID:
19914828
22.

A novel 5-lipoxygenase-activating protein inhibitor, AM679, reduces inflammation in the respiratory syncytial virus-infected mouse eye.

Musiyenko A, Correa L, Stock N, Hutchinson JH, Lorrain DS, Bain G, Evans JF, Barik S.

Clin Vaccine Immunol. 2009 Nov;16(11):1654-9. doi: 10.1128/CVI.00220-09. Epub 2009 Sep 16.

23.

Pharmacological characterization of 3-[3-tert-butylsulfanyl-1-[4-(6-methoxy-pyridin-3-yl)-benzyl]-5-(pyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethyl-propionic acid (AM103), a novel selective 5-lipoxygenase-activating protein inhibitor that reduces acute and chronic inflammation.

Lorrain DS, Bain G, Correa LD, Chapman C, Broadhead AR, Santini AM, Prodanovich P, Darlington JV, Hutchinson JH, King C, Lee C, Baccei C, Li Y, Arruda JM, Evans JF.

J Pharmacol Exp Ther. 2009 Dec;331(3):1042-50. doi: 10.1124/jpet.109.158089. Epub 2009 Sep 11.

PMID:
19749079
24.

5-lipoxygenase-activating protein inhibitors: development of 3-[3-tert-butylsulfanyl-1-[4-(6-methoxy-pyridin-3-yl)-benzyl]-5-(pyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethyl-propionic acid (AM103).

Hutchinson JH, Li Y, Arruda JM, Baccei C, Bain G, Chapman C, Correa L, Darlington J, King CD, Lee C, Lorrain D, Prodanovich P, Rong H, Santini A, Stock N, Prasit P, Evans JF.

J Med Chem. 2009 Oct 8;52(19):5803-15. doi: 10.1021/jm900945d.

PMID:
19739647
25.

Novel tricyclic antagonists of the prostaglandin D2 receptor DP2 with efficacy in a murine model of allergic rhinitis.

Stearns BA, Baccei C, Bain G, Broadhead A, Clark RC, Coate H, Evans JF, Fagan P, Hutchinson JH, King C, Lee C, Lorrain DS, Prasit P, Prodanovich P, Santini A, Scott JM, Stock NS, Truong YP.

Bioorg Med Chem Lett. 2009 Aug 15;19(16):4647-51. doi: 10.1016/j.bmcl.2009.06.085. Epub 2009 Jun 25.

PMID:
19608418
26.

Substituted 2,2-bisaryl-bicycloheptanes as novel and potent inhibitors of 5-lipoxygenase activating protein.

Macdonald D, Brideau C, Chan CC, Falgueyret JP, Frenette R, Guay J, Hutchinson JH, Perrier H, Prasit P, Riendeau D, Tagari P, Thérien M, Young RN, Girard Y.

Bioorg Med Chem Lett. 2008 Mar 15;18(6):2023-7. doi: 10.1016/j.bmcl.2008.01.105. Epub 2008 Feb 2.

PMID:
18276139
27.

What's all the FLAP about?: 5-lipoxygenase-activating protein inhibitors for inflammatory diseases.

Evans JF, Ferguson AD, Mosley RT, Hutchinson JH.

Trends Pharmacol Sci. 2008 Feb;29(2):72-8. doi: 10.1016/j.tips.2007.11.006. Epub 2008 Jan 9. Review.

PMID:
18187210
28.

Diaryl substituted pyrazoles as potent CCR2 receptor antagonists.

Pinkerton AB, Huang D, Cube RV, Hutchinson JH, Struthers M, Ayala JM, Vicario PP, Patel SR, Wisniewski T, DeMartino JA, Vernier JM.

Bioorg Med Chem Lett. 2007 Feb 1;17(3):807-13. Epub 2006 Oct 25.

PMID:
17088058
29.

Biphenyl-indanones: allosteric potentiators of the metabotropic glutamate subtype 2 receptor.

Bonnefous C, Vernier JM, Hutchinson JH, Gardner MF, Cramer M, James JK, Rowe BA, Daggett LP, Schaffhauser H, Kamenecka TM.

Bioorg Med Chem Lett. 2005 Oct 1;15(19):4354-8.

PMID:
16046122
30.

Benzazoles as allosteric potentiators of metabotropic glutamate receptor 2 (mGluR2): efficacy in an animal model for schizophrenia.

Govek SP, Bonnefous C, Hutchinson JH, Kamenecka T, McQuiston J, Pracitto R, Zhao LX, Gardner MF, James JK, Daggett LP, Rowe BA, Schaffhauser H, Bristow LJ, Campbell UC, Rodriguez DE, Vernier JM.

Bioorg Med Chem Lett. 2005 Sep 15;15(18):4068-72.

PMID:
16005222
31.

3-(2-Ethoxy-4-{4-[3-hydroxy-2-methyl-4-(3-methylbutanoyl)phenoxy]butoxy}phenyl)propanoic acid: a brain penetrant allosteric potentiator at the metabotropic glutamate receptor 2 (mGluR2).

Cube RV, Vernier JM, Hutchinson JH, Gardner MF, James JK, Rowe BA, Schaffhauser H, Daggett L, Pinkerton AB.

Bioorg Med Chem Lett. 2005 May 2;15(9):2389-93.

PMID:
15837331
32.

Allosteric potentiators of the metabotropic glutamate receptor 2 (mGlu2). Part 3: Identification and biological activity of indanone containing mGlu2 receptor potentiators.

Pinkerton AB, Cube RV, Hutchinson JH, James JK, Gardner MF, Rowe BA, Schaffhauser H, Rodriguez DE, Campbell UC, Daggett LP, Vernier JM.

Bioorg Med Chem Lett. 2005 Mar 15;15(6):1565-71.

PMID:
15745798
33.

Dipyridyl amides: potent metabotropic glutamate subtype 5 (mGlu5) receptor antagonists.

Bonnefous C, Vernier JM, Hutchinson JH, Chung J, Reyes-Manalo G, Kamenecka T.

Bioorg Med Chem Lett. 2005 Feb 15;15(4):1197-200.

PMID:
15686941
34.

Allosteric potentiators of the metabotropic glutamate receptor 2 (mGlu2). Part 2: 4-thiopyridyl acetophenones as non-tetrazole containing mGlu2 receptor potentiators.

Pinkerton AB, Cube RV, Hutchinson JH, James JK, Gardner MF, Schaffhauser H, Rowe BA, Daggett LP, Vernier JM.

Bioorg Med Chem Lett. 2004 Dec 6;14(23):5867-72.

PMID:
15501058
35.

Allosteric potentiators of the metabotropic glutamate receptor 2 (mGlu2). Part 1: Identification and synthesis of phenyl-tetrazolyl acetophenones.

Pinkerton AB, Cube RV, Hutchinson JH, Rowe BA, Schaffhauser H, Zhao X, Daggett LP, Vernier JM.

Bioorg Med Chem Lett. 2004 Nov 1;14(21):5329-32.

PMID:
15454221
36.

Pyrimidine methyl anilines: selective potentiators for the metabotropic glutamate 2 receptor.

Hu E, Chua PC, Tehrani L, Nagasawa JY, Pinkerton AB, Rowe BA, Vernier JM, Hutchinson JH, Cosford ND.

Bioorg Med Chem Lett. 2004 Oct 18;14(20):5071-4.

PMID:
15380201
37.

Nonpeptide alphavbeta3 antagonists. Part 11: discovery and preclinical evaluation of potent alphavbeta3 antagonists for the prevention and treatment of osteoporosis.

Coleman PJ, Brashear KM, Askew BC, Hutchinson JH, McVean CA, Duong LT, Feuston BP, Fernandez-Metzler C, Gentile MA, Hartman GD, Kimmel DB, Leu CT, Lipfert L, Merkle K, Pennypacker B, Prueksaritanont T, Rodan GA, Wesolowski GA, Rodan SB, Duggan ME.

J Med Chem. 2004 Sep 23;47(20):4829-37.

PMID:
15369386
38.

Nonpeptide alpha V beta 3 antagonists. Part 10: In vitro and in vivo evaluation of a potent 7-methyl substituted tetrahydro-[1,8]naphthyridine derivative.

Breslin MJ, Duggan ME, Halczenko W, Hartman GD, Duong LT, Fernandez-Metzler C, Gentile MA, Kimmel DB, Leu CT, Merkle K, Prueksaritanont T, Rodan GA, Rodan SB, Hutchinson JH.

Bioorg Med Chem Lett. 2004 Sep 6;14(17):4515-8.

PMID:
15357983
39.

Nonpeptide alpha V beta 3 antagonists. Part 9: Improved pharmacokinetic profile through the use of an aliphatic, des-amide backbone.

Whitman DB, Askew BC, Duong LT, Fernandez-Metzler C, Halczenko W, Hartman GD, Hutchinson JH, Leu CT, Prueksaritanont T, Rodan GA, Rodan SB, Duggan ME.

Bioorg Med Chem Lett. 2004 Sep 6;14(17):4411-5.

PMID:
15357963
40.

Non-peptide alpha v beta 3 antagonists. Part 7: 3-Substituted tetrahydro-naphthyridine derivatives.

Wang J, Breslin MJ, Coleman PJ, Duggan ME, Hunt CA, Hutchinson JH, Leu CT, Rodan SB, Rodan GA, Duong LT, Hartman GD.

Bioorg Med Chem Lett. 2004 Feb 23;14(4):1049-52.

PMID:
15013021
41.

Disposition of a novel and potent alpha(v)beta3 antagonist in animals, and extrapolation to man.

Prueksaritanont T, Fernandez-Metzler C, Meng Y, Barrish A, Halczenko W, Rodan SB, Hutchinson JH, Duggan ME, Lin JH.

Xenobiotica. 2004 Jan;34(1):103-15.

PMID:
14742139
42.

Nonpeptide alphavbeta3 antagonists. 8. In vitro and in vivo evaluation of a potent alphavbeta3 antagonist for the prevention and treatment of osteoporosis.

Hutchinson JH, Halczenko W, Brashear KM, Breslin MJ, Coleman PJ, Duong LT, Fernandez-Metzler C, Gentile MA, Fisher JE, Hartman GD, Huff JR, Kimmel DB, Leu CT, Meissner RS, Merkle K, Nagy R, Pennypacker B, Perkins JJ, Prueksaritanont T, Rodan GA, Varga SL, Wesolowski GA, Zartman AE, Rodan SB, Duggan ME.

J Med Chem. 2003 Oct 23;46(22):4790-8.

PMID:
14561098
43.

Non-peptide alphavbeta3 antagonists. Part 6: design and synthesis of alphavbeta3 antagonists containing a pyridone or pyrazinone central scaffold.

Breslin MJ, Duggan ME, Halczenko W, Fernandez-Metzler C, Hunt CA, Leu CT, Merkle KM, Naylor-Olsen AM, Prueksaritanont T, Stump G, Wallace A, Rodan SB, Hutchinson JH.

Bioorg Med Chem Lett. 2003 May 19;13(10):1809-12.

PMID:
12729670
44.

Non-peptide alpha(v)beta(3) antagonists. Part 5: identification of potent RGD mimetics incorporating 2-aryl beta-amino acids as aspartic acid replacements.

Brashear KM, Hunt CA, Kucer BT, Duggan ME, Hartman GD, Rodan GA, Rodan SB, Leu CT, Prueksaritanont T, Fernandez-Metzler C, Barrish A, Homnick CF, Hutchinson JH, Coleman PJ.

Bioorg Med Chem Lett. 2002 Dec 2;12(23):3483-6.

PMID:
12419389
45.

Non-peptide alpha(v)beta(3) antagonists. Part 4: potent and orally bioavailable chain-shortened RGD mimetics.

Coleman PJ, Askew BC, Hutchinson JH, Whitman DB, Perkins JJ, Hartman GD, Rodan GA, Leu CT, Prueksaritanont T, Fernandez-Metzler C, Merkle KM, Lynch R, Lynch JJ, Rodan SB, Duggan ME.

Bioorg Med Chem Lett. 2002 Sep 2;12(17):2463-5.

PMID:
12161158
46.

Non-peptide alpha(v)beta(3) antagonists. Part 3: identification of potent RGD mimetics incorporating novel beta-amino acids as aspartic acid replacements.

Coleman PJ, Brashear KM, Hunt CA, Hoffman WF, Hutchinson JH, Breslin MJ, McVean CA, Askew BC, Hartman GD, Rodan SB, Rodan GA, Leu CT, Prueksaritanont T, Fernandez-Metzler C, Ma B, Libby LA, Merkle KM, Stump GL, Wallace AA, Lynch JJ, Lynch R, Duggan ME.

Bioorg Med Chem Lett. 2002 Jan 7;12(1):31-4.

PMID:
11738567
47.

Discovery and initial structure-activity relationships of trisubstituted ureas as thrombin receptor (PAR-1) antagonists.

Barrow JC, Nantermet PG, Selnick HG, Glass KL, Ngo PL, Young MB, Pellicore JM, Breslin MJ, Hutchinson JH, Freidinger RM, Condra C, Karczewski J, Bednar RA, Gaul SL, Stern A, Gould R, Connolly TM.

Bioorg Med Chem Lett. 2001 Oct 22;11(20):2691-6.

PMID:
11591503
48.

Diaryl ether inhibitors of farnesyl-protein transferase.

Mactough SC, Desolms SJ, Shaw AW, Abrams MT, Ciccarone TM, Davide JP, Hamilton KA, Hutchinson JH, Koblan KS, Kohl NE, Lobell RB, Robinson RG, Graham SL.

Bioorg Med Chem Lett. 2001 May 21;11(10):1257-60.

PMID:
11392531
49.

Nonpeptide GPIIB/IIIA receptor antagonists. Part 21: C-6 flexibility and amide bond orientation are important factors in determining the affinity of compounds for activated or resting platelet receptors.

Egbertson MS, Bednar B, Askew BC, Bednar RA, Brashear K, Breslin MJ, Duggan ME, Fisher TE, Halczenko W, Hutchinson JH, Ihle N, Prugh JD, Wai JS, Gould RJ, Hartman GD.

Bioorg Med Chem Lett. 2000 Sep 4;10(17):1943-8.

PMID:
10987423
50.

N-arylpiperazinone inhibitors of farnesyltransferase: discovery and biological activity.

Williams TM, Bergman JM, Brashear K, Breslin MJ, Dinsmore CJ, Hutchinson JH, MacTough SC, Stump CA, Wei DD, Zartman CB, Bogusky MJ, Culberson JC, Buser-Doepner C, Davide J, Greenberg IB, Hamilton KA, Koblan KS, Kohl NE, Liu D, Lobell RB, Mosser SD, O'Neill TJ, Rands E, Schaber MD, Huff JR, et al.

J Med Chem. 1999 Sep 23;42(19):3779-84. No abstract available.

PMID:
10508426

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