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Items: 1 to 50 of 52

1.

Hit-to-Lead Optimization and Discovery of 5-((5-([1,1'-Biphenyl]-4-yl)-6-chloro-1H-benzo[d]imidazol-2-yl)oxy)-2-methylbenzoic Acid (MK-3903): A Novel Class of Benzimidazole-Based Activators of AMP-Activated Protein Kinase.

Lan P, Romero FA, Wodka D, Kassick AJ, Dang Q, Gibson T, Cashion D, Zhou G, Chen Y, Zhang X, Zhang A, Li Y, Trujillo ME, Shao Q, Wu M, Xu S, He H, MacKenna D, Staunton J, Chapman KT, Weber A, Sebhat IK, Makara GM.

J Med Chem. 2017 Nov 9;60(21):9040-9052. doi: 10.1021/acs.jmedchem.7b01344. Epub 2017 Oct 25.

PMID:
29035567
2.

Discovery of novel, potent, selective, and orally active human glucagon receptor antagonists containing a pyrazole core.

Shen DM, Brady EJ, Candelore MR, Dallas-Yang Q, Ding VD, Feeney WP, Jiang G, McCann ME, Mock S, Qureshi SA, Saperstein R, Shen X, Tong X, Tota LM, Wright MJ, Yang X, Zheng S, Chapman KT, Zhang BB, Tata JR, Parmee ER.

Bioorg Med Chem Lett. 2011 Jan 1;21(1):76-81. doi: 10.1016/j.bmcl.2010.11.074. Epub 2010 Nov 21.

PMID:
21147532
3.

Design and synthesis of prolylcarboxypeptidase (PrCP) inhibitors to validate PrCP as a potential target for obesity.

Zhou C, Garcia-Calvo M, Pinto S, Lombardo M, Feng Z, Bender K, Pryor KD, Bhatt UR, Chabin RM, Geissler WM, Shen Z, Tong X, Zhang Z, Wong KK, Roy RS, Chapman KT, Yang L, Xiong Y.

J Med Chem. 2010 Oct 14;53(19):7251-63. doi: 10.1021/jm101013m.

PMID:
20857914
4.

Design and synthesis of a new class of malonyl-CoA decarboxylase inhibitors with anti-obesity and anti-diabetic activities.

Tang H, Yan Y, Feng Z, de Jesus RK, Yang L, Levorse DA, Owens KA, Akiyama TE, Bergeron R, Castriota GA, Doebber TW, Ellsworth KP, Lassman ME, Li C, Wu MS, Zhang BB, Chapman KT, Mills SG, Berger JP, Pasternak A.

Bioorg Med Chem Lett. 2010 Oct 15;20(20):6088-92. doi: 10.1016/j.bmcl.2010.08.047. Epub 2010 Aug 20.

PMID:
20832306
5.

Application of affinity selection/mass spectrometry to determine the structural isomer of parnafungins responsible for binding polyadenosine polymerase.

Adam GC, Parish CA, Wisniewski D, Meng J, Liu M, Calati K, Stein BD, Athanasopoulos J, Liberator P, Roemer T, Harris G, Chapman KT.

J Am Chem Soc. 2008 Dec 10;130(49):16704-10. doi: 10.1021/ja805531w.

PMID:
19049464
6.

Synthesis of novel HIV protease inhibitors (PI) with activity against PI-resistant virus.

Raghavan S, Lu Z, Beeson T, Chapman KT, Schleif WA, Olsen DB, Stahlhut M, Rutkowski CA, Gabryelski L, Emini E, Tata JR.

Bioorg Med Chem Lett. 2007 Oct 1;17(19):5432-6. Epub 2007 Jul 31.

PMID:
17692518
7.

Affinity-based ranking of ligands for DPP-4 from mixtures.

Adam GC, Meng J, Athanasopoulos J, Zhang X, Chapman KT.

Bioorg Med Chem Lett. 2007 May 1;17(9):2404-7. Epub 2007 Feb 17.

PMID:
17337342
8.

The discovery of a potent and selective lethal factor inhibitor for adjunct therapy of anthrax infection.

Xiong Y, Wiltsie J, Woods A, Guo J, Pivnichny JV, Tang W, Bansal A, Cummings RT, Cunningham BR, Friedlander AM, Douglas CM, Salowe SP, Zaller DM, Scolnick EM, Schmatz DM, Bartizal K, Hermes JD, MacCoss M, Chapman KT.

Bioorg Med Chem Lett. 2006 Feb 15;16(4):964-8. Epub 2005 Dec 9.

PMID:
16338135
9.

Discovery of novel, potent, and orally active spiro-urea human glucagon receptor antagonists.

Shen DM, Zhang F, Brady EJ, Candelore MR, Dallas-Yang Q, Ding VD, Dragovic J, Feeney WP, Jiang G, McCann PE, Mock S, Qureshi SA, Saperstein R, Shen X, Tamvakopoulos C, Tong X, Tota LM, Wright MJ, Yang X, Zheng S, Chapman KT, Zhang BB, Tata JR, Parmee ER.

Bioorg Med Chem Lett. 2005 Oct 15;15(20):4564-9.

PMID:
16102966
10.

The target of ezetimibe is Niemann-Pick C1-Like 1 (NPC1L1).

Garcia-Calvo M, Lisnock J, Bull HG, Hawes BE, Burnett DA, Braun MP, Crona JH, Davis HR Jr, Dean DC, Detmers PA, Graziano MP, Hughes M, Macintyre DE, Ogawa A, O'neill KA, Iyer SP, Shevell DE, Smith MM, Tang YS, Makarewicz AM, Ujjainwalla F, Altmann SW, Chapman KT, Thornberry NA.

Proc Natl Acad Sci U S A. 2005 Jun 7;102(23):8132-7. Epub 2005 May 31.

11.

Anthrax lethal factor inhibition.

Shoop WL, Xiong Y, Wiltsie J, Woods A, Guo J, Pivnichny JV, Felcetto T, Michael BF, Bansal A, Cummings RT, Cunningham BR, Friedlander AM, Douglas CM, Patel SB, Wisniewski D, Scapin G, Salowe SP, Zaller DM, Chapman KT, Scolnick EM, Schmatz DM, Bartizal K, MacCoss M, Hermes JD.

Proc Natl Acad Sci U S A. 2005 May 31;102(22):7958-63. Epub 2005 May 23.

12.

Discovery and investigation of a novel class of thiophene-derived antagonists of the human glucagon receptor.

Duffy JL, Kirk BA, Konteatis Z, Campbell EL, Liang R, Brady EJ, Candelore MR, Ding VD, Jiang G, Liu F, Qureshi SA, Saperstein R, Szalkowski D, Tong S, Tota LM, Xie D, Yang X, Zafian P, Zheng S, Chapman KT, Zhang BB, Tata JR.

Bioorg Med Chem Lett. 2005 Mar 1;15(5):1401-5.

PMID:
15713396
13.

A novel glucagon receptor antagonist inhibits glucagon-mediated biological effects.

Qureshi SA, Rios Candelore M, Xie D, Yang X, Tota LM, Ding VD, Li Z, Bansal A, Miller C, Cohen SM, Jiang G, Brady E, Saperstein R, Duffy JL, Tata JR, Chapman KT, Moller DE, Zhang BB.

Diabetes. 2004 Dec;53(12):3267-73.

14.

P1' oxadiazole protease inhibitors with excellent activity against native and protease inhibitor-resistant HIV-1.

Kim RM, Rouse EA, Chapman KT, Schleif WA, Olsen DB, Stahlhut M, Rutkowski CA, Emini EA, Tata JR.

Bioorg Med Chem Lett. 2004 Sep 20;14(18):4651-4.

PMID:
15324882
15.

Antagonists of human CCR5 receptor containing 4-(pyrazolyl)piperidine side chains. Part 3: SAR studies on the benzylpyrazole segment.

Shu M, Loebach JL, Parker KA, Mills SG, Chapman KT, Shen DM, Malkowitz L, Springer MS, Gould SL, DeMartino JA, Siciliano SJ, Salvo JD, Lyons K, Pivnichny JV, Kwei GY, Carella A, Carver G, Holmes K, Schleif WA, Danzeisen R, Hazuda D, Kessler J, Lineberger J, Miller MD, Emini EA.

Bioorg Med Chem Lett. 2004 Feb 23;14(4):947-52.

PMID:
15012999
16.

Antagonists of human CCR5 receptor containing 4-(pyrazolyl)piperidine side chains. Part 2: Discovery of potent, selective, and orally bioavailable compounds.

Shen DM, Shu M, Willoughby CA, Shah S, Lynch CL, Hale JJ, Mills SG, Chapman KT, Malkowitz L, Springer MS, Gould SL, DeMartino JA, Siciliano SJ, Lyons K, Pivnichny JV, Kwei GY, Carella A, Carver G, Holmes K, Schleif WA, Danzeisen R, Hazuda D, Kessler J, Lineberger J, Miller MD, Emini EA.

Bioorg Med Chem Lett. 2004 Feb 23;14(4):941-5.

PMID:
15012998
17.

Antagonists of human CCR5 receptor containing 4-(pyrazolyl)piperidine side chains. Part 1: Discovery and SAR study of 4-pyrazolylpiperidine side chains.

Shen DM, Shu M, Mills SG, Chapman KT, Malkowitz L, Springer MS, Gould SL, DeMartino JA, Siciliano SJ, Kwei GY, Carella A, Carver G, Holmes K, Schleif WA, Danzeisen R, Hazuda D, Kessler J, Lineberger J, Miller MD, Emini EA.

Bioorg Med Chem Lett. 2004 Feb 23;14(4):935-9.

PMID:
15012997
18.

Novel 3,4-dihydroquinolin-2(1H)-one inhibitors of human glycogen phosphorylase a.

Rosauer KG, Ogawa AK, Willoughby CA, Ellsworth KP, Geissler WM, Myers RW, Deng Q, Chapman KT, Harris G, Moller DE.

Bioorg Med Chem Lett. 2003 Dec 15;13(24):4385-8.

PMID:
14643331
19.

Novel HIV-1 protease inhibitors active against multiple PI-resistant viral strains: coadministration with indinavir.

Kevin NJ, Duffy JL, Kirk BA, Chapman KT, Schleif WA, Olsen DB, Stahlhut M, Rutkowski CA, Kuo LC, Jin L, Lin JH, Emini EA, Tata JR.

Bioorg Med Chem Lett. 2003 Nov 17;13(22):4027-30.

PMID:
14592500
20.

Glucose-lowering in a db/db mouse model by dihydropyridine diacid glycogen phosphorylase inhibitors.

Ogawa AK, Willoughby CA, Bergeron R, Ellsworth KP, Geissler WM, Myers RW, Yao J, Harris G, Chapman KT.

Bioorg Med Chem Lett. 2003 Oct 20;13(20):3405-8.

PMID:
14505637
21.

HIV-1 protease inhibitors with picomolar potency against PI-resistant HIV-1 by modification of the P1' substituent.

Duffy JL, Kirk BA, Kevin NJ, Chapman KT, Schleif WA, Olsen DB, Stahlhut M, Rutkowski CA, Kuo LC, Jin L, Lin JH, Emini EA, Tata JR.

Bioorg Med Chem Lett. 2003 Oct 6;13(19):3323-6.

PMID:
12951118
22.

The design, synthesis and evaluation of novel HIV-1 protease inhibitors with high potency against PI-resistant viral strains.

Zhang F, Chapman KT, Schleif WA, Olsen DB, Stahlhut M, Rutkowski CA, Kuo LC, Jin L, Lin JH, Emini EA, Tata JR.

Bioorg Med Chem Lett. 2003 Aug 4;13(15):2573-6.

PMID:
12852969
23.

HIV protease inhibitors with picomolar potency against PI-Resistant HIV-1 by extension of the P3 substituent.

Duffy JL, Rano TA, Kevin NJ, Chapman KT, Schleif WA, Olsen DB, Stahlhut M, Rutkowski CA, Kuo LC, Jin L, Lin JH, Emini EA, Tata JR.

Bioorg Med Chem Lett. 2003 Aug 4;13(15):2569-72.

PMID:
12852968
24.

CCR5 antagonists: 3-(pyrrolidin-1-yl)propionic acid analogues with potent anti-HIV activity.

Lynch CL, Hale JJ, Budhu RJ, Gentry AL, Finke PE, Caldwell CG, Mills SG, MacCoss M, Shen DM, Chapman KT, Malkowitz L, Springer MS, Gould SL, DeMartino JA, Siciliano SJ, Cascieri MA, Carella A, Carver G, Holmes K, Schleif WA, Danzeisen R, Hazuda D, Kessler J, Lineberger J, Miller M, Emini E.

Org Lett. 2003 Jul 10;5(14):2473-5.

PMID:
12841758
25.

1,3,4 Trisubstituted pyrrolidine CCR5 receptor antagonists bearing 4-aminoheterocycle substituted piperidine side chains.

Willoughby CA, Rosauer KG, Hale JJ, Budhu RJ, Mills SG, Chapman KT, MacCoss M, Malkowitz L, Springer MS, Gould SL, DeMartino JA, Siciliano SJ, Cascieri MA, Carella A, Carver G, Holmes K, Schleif WA, Danzeisen R, Hazuda D, Kessler J, Lineberger J, Miller M, Emini EA.

Bioorg Med Chem Lett. 2003 Feb 10;13(3):427-31.

PMID:
12565944
26.

1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists: modifications of the arylpropylpiperidine side chains.

Lynch CL, Willoughby CA, Hale JJ, Holson EJ, Budhu RJ, Gentry AL, Rosauer KG, Caldwell CG, Chen P, Mills SG, MacCoss M, Berk S, Chen L, Chapman KT, Malkowitz L, Springer MS, Gould SL, DeMartino JA, Siciliano SJ, Cascieri MA, Carella A, Carver G, Holmes K, Schleif WA, Danzeisen R, Hazuda D, Kessler J, Lineberger J, Miller M, Emini EA.

Bioorg Med Chem Lett. 2003 Jan 6;13(1):119-23.

PMID:
12467630
27.

1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 4: synthesis of N-1 acidic functionality affording analogues with enhanced antiviral activity against HIV.

Lynch CL, Hale JJ, Budhu RJ, Gentry AL, Mills SG, Chapman KT, MacCoss M, Malkowitz L, Springer MS, Gould SL, DeMartino JA, Siciliano SJ, Cascieri MA, Carella A, Carver G, Holmes K, Schleif WA, Danzeisen R, Hazuda D, Kessler J, Lineberger J, Miller M, Emini EA.

Bioorg Med Chem Lett. 2002 Oct 21;12(20):3001-4.

PMID:
12270193
28.

Combinatorial library of indinavir analogues: replacement for the aminoindanol at P2'.

Raghavan S, Yang Z, Mosley RT, Schleif WA, Gabryelski L, Olsen DB, Stahlhut M, Kuo LC, Emini EA, Chapman KT, Tata JR.

Bioorg Med Chem Lett. 2002 Oct 21;12(20):2855-8.

PMID:
12270162
29.

Synthesis and activity of novel HIV protease inhibitors with improved potency against multiple PI-resistant viral strains.

Duffy JL, Kevin NJ, Kirk BA, Chapman KT, Schleif WA, Olsen DB, Stahlhut M, Rutkowski CA, Kuo LC, Jin L, Lin JH, Emini EA, Tata JR.

Bioorg Med Chem Lett. 2002 Sep 2;12(17):2423-6.

PMID:
12161148
30.

Indinavir analogues with blocked metabolism sites as HIV protease inhibitors with improved pharmacological profiles and high potency against PI-resistant viral strains.

Cheng Y, Zhang F, Rano TA, Lu Z, Schleif WA, Gabryelski L, Olsen DB, Stahlhut M, Rutkowski CA, Lin JH, Jin L, Emini EA, Chapman KT, Tata JR.

Bioorg Med Chem Lett. 2002 Sep 2;12(17):2419-22.

PMID:
12161147
31.

Discovery of potent, selective human granzyme B inhibitors that inhibit CTL mediated apoptosis.

Willoughby CA, Bull HG, Garcia-Calvo M, Jiang J, Chapman KT, Thornberry NA.

Bioorg Med Chem Lett. 2002 Aug 19;12(16):2197-200.

PMID:
12127536
32.

A combinatorial library of indinavir analogues and its in vitro and in vivo studies.

Cheng Y, Rano TA, Huening TT, Zhang F, Lu Z, Schleif WA, Gabryelski L, Olsen DB, Stahlhut M, Kuo LC, Lin JH, Xu X, Jin L, Olah TV, McLoughlin DA, King RC, Chapman KT, Tata JR.

Bioorg Med Chem Lett. 2002 Feb 25;12(4):529-32.

PMID:
11844665
33.

Combinatorial synthesis of 3-(amidoalkyl) and 3-(aminoalkyl)-2-arylindole derivatives: discovery of potent ligands for a variety of G-protein coupled receptors.

Willoughby CA, Hutchins SM, Rosauer KG, Dhar MJ, Chapman KT, Chicchi GG, Sadowski S, Weinberg DH, Patel S, Malkowitz L, Di Salvo J, Pacholok SG, Cheng K.

Bioorg Med Chem Lett. 2002 Jan 7;12(1):93-6.

PMID:
11738581
34.

Combinatorial synthesis of CCR5 antagonists.

Willoughby CA, Berk SC, Rosauer KG, Degrado S, Chapman KT, Gould SL, Springer MS, Malkowitz L, Schleif WA, Hazuda D, Miller M, Kessler J, Danzeisen R, Holmes K, Lineberger J, Carella A, Carver G, Emini EA.

Bioorg Med Chem Lett. 2001 Dec 17;11(24):3137-41.

PMID:
11720860
35.

Solid phase synthesis of indinavir and its analogues.

Cheng Y, Lu Z, Chapman KT, Tata JR.

J Comb Chem. 2000 Sep-Oct;2(5):445-6. No abstract available.

PMID:
11029167
36.

Versatile and efficient solid-phase syntheses of pyrazoles and isoxazoles.

Shen DM, Shu M, Chapman KT.

Org Lett. 2000 Sep 7;2(18):2789-92.

PMID:
10964366
37.

Combinatorial diversification of indinavir: in vivo mixture dosing of an HIV protease inhibitor library.

Rano TA, Cheng Y, Huening TT, Zhang F, Schleif WA, Gabryelski L, Olsen DB, Kuo LC, Lin JH, Xu X, Olah TV, McLoughlin DA, King R, Chapman KT, Tata JR.

Bioorg Med Chem Lett. 2000 Jul 17;10(14):1527-30.

PMID:
10915042
38.

Determination of caspase specificities using a peptide combinatorial library.

Thornberry NA, Chapman KT, Nicholson DW.

Methods Enzymol. 2000;322:100-10. No abstract available.

PMID:
10914008
39.

A combinatorial approach toward the discovery of non-peptide, subtype-selective somatostatin receptor ligands.

Berk SC, Rohrer SP, Degrado SJ, Birzin ET, Mosley RT, Hutchins SM, Pasternak A, Schaeffer JM, Underwood DJ, Chapman KT.

J Comb Chem. 1999 Sep-Oct;1(5):388-96.

PMID:
10748735
40.

Rapid identification of subtype-selective agonists of the somatostatin receptor through combinatorial chemistry.

Rohrer SP, Birzin ET, Mosley RT, Berk SC, Hutchins SM, Shen DM, Xiong Y, Hayes EC, Parmar RM, Foor F, Mitra SW, Degrado SJ, Shu M, Klopp JM, Cai SJ, Blake A, Chan WW, Pasternak A, Yang L, Patchett AA, Smith RG, Chapman KT, Schaeffer JM.

Science. 1998 Oct 23;282(5389):737-40. Erratum in: Science 1998 Nov 27;282(5394):1646.

41.

A combinatorial approach defines specificities of members of the caspase family and granzyme B. Functional relationships established for key mediators of apoptosis.

Thornberry NA, Rano TA, Peterson EP, Rasper DM, Timkey T, Garcia-Calvo M, Houtzager VM, Nordstrom PA, Roy S, Vaillancourt JP, Chapman KT, Nicholson DW.

J Biol Chem. 1997 Jul 18;272(29):17907-11.

42.

Combinatorial chemistry searching for a winning combination

Joyce GF, Still WC, Chapman KT.

Curr Opin Chem Biol. 1997 Jun;1(1):3-4. No abstract available.

PMID:
9667845
43.

Inhibition of stromelysin-1 (MMP-3) by P1'-biphenylylethyl carboxyalkyl dipeptides.

Esser CK, Bugianesi RL, Caldwell CG, Chapman KT, Durette PL, Girotra NN, Kopka IE, Lanza TJ, Levorse DA, MacCoss M, Owens KA, Ponpipom MM, Simeone JP, Harrison RK, Niedzwiecki L, Becker JW, Marcy AI, Axel MG, Christen AJ, McDonnell J, Moore VL, Olszewski JM, Saphos C, Visco DM, Hagmann WK, et al.

J Med Chem. 1997 Mar 14;40(6):1026-40.

PMID:
9083493
44.

A combinatorial approach for determining protease specificities: application to interleukin-1beta converting enzyme (ICE).

Rano TA, Timkey T, Peterson EP, Rotonda J, Nicholson DW, Becker JW, Chapman KT, Thornberry NA.

Chem Biol. 1997 Feb;4(2):149-55.

45.

Dendrimer-supported combinatorial chemistry.

Kim RM, Manna M, Hutchins SM, Griffin PR, Yates NA, Bernick AM, Chapman KT.

Proc Natl Acad Sci U S A. 1996 Sep 17;93(19):10012-7.

46.

Proteoglycan-degrading activity of human stromelysin-1 and leukocyte elastase in rabbit joints. Quantitation of proteoglycan and a stromelysin-induced HABR fragment of aggrecan in synovial fluid and cartilage.

Olszewski JM, Moore VL, McDonnell J, Williams H, Saphos CA, Green BG, Knight WB, Chapman KT, Hagmann WK, Dorn CP, Hale JJ, Mumford RA.

Connect Tissue Res. 1996;33(4):291-9.

PMID:
8834447
47.

A synthetic inhibitor of interleukin-1 beta converting enzyme prevents endotoxin-induced interleukin-1 beta production in vitro and in vivo.

Fletcher DS, Agarwal L, Chapman KT, Chin J, Egger LA, Limjuco G, Luell S, MacIntyre DE, Peterson EP, Thornberry NA, et al.

J Interferon Cytokine Res. 1995 Mar;15(3):243-8.

PMID:
7584670
48.

Inactivation of interleukin-1 beta converting enzyme by peptide (acyloxy)methyl ketones.

Thornberry NA, Peterson EP, Zhao JJ, Howard AD, Griffin PR, Chapman KT.

Biochemistry. 1994 Apr 5;33(13):3934-40.

PMID:
8142397
49.

Studies on the kinetic and chemical mechanism of inhibition of stromelysin by an N-(carboxyalkyl)dipeptide.

Izquierdo-Martin M, Chapman KT, Hagmann WK, Stein RL.

Biochemistry. 1994 Feb 15;33(6):1356-65.

PMID:
8312254
50.

Inhibition of matrix metalloproteinases by N-carboxyalkyl peptides.

Chapman KT, Kopka IE, Durette PL, Esser CK, Lanza TJ, Izquierdo-Martin M, Niedzwiecki L, Chang B, Harrison RK, Kuo DW, et al.

J Med Chem. 1993 Dec 24;36(26):4293-301.

PMID:
8277511

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