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Items: 1 to 50 of 54

1.

Discovery of GSK1070916, a potent and selective inhibitor of Aurora B/C kinase.

Adams ND, Adams JL, Burgess JL, Chaudhari AM, Copeland RA, Donatelli CA, Drewry DH, Fisher KE, Hamajima T, Hardwicke MA, Huffman WF, Koretke-Brown KK, Lai ZV, McDonald OB, Nakamura H, Newlander KA, Oleykowski CA, Parrish CA, Patrick DR, Plant R, Sarpong MA, Sasaki K, Schmidt SJ, Silva DJ, Sutton D, Tang J, Thompson CS, Tummino PJ, Wang JC, Xiang H, Yang J, Dhanak D.

J Med Chem. 2010 May 27;53(10):3973-4001. doi: 10.1021/jm901870q.

PMID:
20420387
2.

An orally active calcium-sensing receptor antagonist that transiently increases plasma concentrations of PTH and stimulates bone formation.

Kumar S, Matheny CJ, Hoffman SJ, Marquis RW, Schultz M, Liang X, Vasko JA, Stroup GB, Vaden VR, Haley H, Fox J, DelMar EG, Nemeth EF, Lago AM, Callahan JF, Bhatnagar P, Huffman WF, Gowen M, Yi B, Danoff TM, Fitzpatrick LA.

Bone. 2010 Feb;46(2):534-42. doi: 10.1016/j.bone.2009.09.028. Epub 2009 Sep 26.

PMID:
19786130
3.

Novel ATP-competitive kinesin spindle protein inhibitors.

Parrish CA, Adams ND, Auger KR, Burgess JL, Carson JD, Chaudhari AM, Copeland RA, Diamond MA, Donatelli CA, Duffy KJ, Faucette LF, Finer JT, Huffman WF, Hugger ED, Jackson JR, Knight SD, Luo L, Moore ML, Newlander KA, Ridgers LH, Sakowicz R, Shaw AN, Sung CM, Sutton D, Wood KW, Zhang SY, Zimmerman MN, Dhanak D.

J Med Chem. 2007 Oct 4;50(20):4939-52. Epub 2007 Aug 29.

PMID:
17725339
4.

Indole naphthyridinones as inhibitors of bacterial enoyl-ACP reductases FabI and FabK.

Seefeld MA, Miller WH, Newlander KA, Burgess WJ, DeWolf WE Jr, Elkins PA, Head MS, Jakas DR, Janson CA, Keller PM, Manley PJ, Moore TD, Payne DJ, Pearson S, Polizzi BJ, Qiu X, Rittenhouse SF, Uzinskas IN, Wallis NG, Huffman WF.

J Med Chem. 2003 Apr 24;46(9):1627-35.

PMID:
12699381
5.

Phenylbutyrates as potent, orally bioavailable vitronectin receptor (integrin alphavbeta3) antagonists.

Miller WH, Manley PJ, Cousins RD, Erhard KF, Heerding DA, Kwon C, Ross ST, Samanen JM, Takata DT, Uzinskas IN, Yuan CC, Haltiwanger RC, Gress CJ, Lark MW, Hwang SM, James IE, Rieman DJ, Willette RN, Yue TL, Azzarano LM, Salyers KL, Smith BR, Ward KW, Johanson KO, Huffman WF.

Bioorg Med Chem Lett. 2003 Apr 17;13(8):1483-6.

PMID:
12668017
6.

Discovery of a novel and potent class of FabI-directed antibacterial agents.

Payne DJ, Miller WH, Berry V, Brosky J, Burgess WJ, Chen E, DeWolf WE Jr, Fosberry AP, Greenwood R, Head MS, Heerding DA, Janson CA, Jaworski DD, Keller PM, Manley PJ, Moore TD, Newlander KA, Pearson S, Polizzi BJ, Qiu X, Rittenhouse SF, Slater-Radosti C, Salyers KL, Seefeld MA, Smyth MG, Takata DT, Uzinskas IN, Vaidya K, Wallis NG, Winram SB, Yuan CC, Huffman WF.

Antimicrob Agents Chemother. 2002 Oct;46(10):3118-24.

7.

Discovery of aminopyridine-based inhibitors of bacterial enoyl-ACP reductase (FabI).

Miller WH, Seefeld MA, Newlander KA, Uzinskas IN, Burgess WJ, Heerding DA, Yuan CC, Head MS, Payne DJ, Rittenhouse SF, Moore TD, Pearson SC, Berry V, DeWolf WE Jr, Keller PM, Polizzi BJ, Qiu X, Janson CA, Huffman WF.

J Med Chem. 2002 Jul 18;45(15):3246-56.

PMID:
12109908
8.

Inhibitors of bacterial enoyl acyl carrier protein reductase (FabI): 2,9-disubstituted 1,2,3,4-tetrahydropyrido[3,4-b]indoles as potential antibacterial agents.

Seefeld MA, Miller WH, Newlander KA, Burgess WJ, Payne DJ, Rittenhouse SF, Moore TD, DeWolf WE Jr, Keller PM, Qiu X, Janson CA, Vaidya K, Fosberry AP, Smyth MG, Jaworski DD, Slater-Radosti C, Huffman WF.

Bioorg Med Chem Lett. 2001 Sep 3;11(17):2241-4.

PMID:
11527706
9.

1,4-Disubstituted imidazoles are potential antibacterial agents functioning as inhibitors of enoyl acyl carrier protein reductase (FabI).

Heerding DA, Chan G, DeWolf WE, Fosberry AP, Janson CA, Jaworski DD, McManus E, Miller WH, Moore TD, Payne DJ, Qiu X, Rittenhouse SF, Slater-Radosti C, Smith W, Takata DT, Vaidya KS, Yuan CC, Huffman WF.

Bioorg Med Chem Lett. 2001 Aug 20;11(16):2061-5.

PMID:
11514139
10.

Antagonism of the osteoclast vitronectin receptor with an orally active nonpeptide inhibitor prevents cancellous bone loss in the ovariectomized rat.

Lark MW, Stroup GB, Dodds RA, Kapadia R, Hoffman SJ, Hwang SM, James IE, Lechowska B, Liang X, Rieman DJ, Salyers KL, Ward K, Smith BR, Miller WH, Huffman WF, Gowen M.

J Bone Miner Res. 2001 Feb;16(2):319-27.

11.

Novel peptidomimetic hematoregulatory compounds.

Heerding DA, Abruzzese M, Alberts D, Burgess J, Callahan JF, Huffman WF, King AG, LoCastro S, DeMarsh P, Pelus LM, Takata JS, Bhatnagar PK.

Bioorg Med Chem Lett. 2000 Mar 20;10(6):531-4.

PMID:
10741547
12.

Discovery of orally active nonpeptide vitronectin receptor antagonists based on a 2-benzazepine Gly-Asp mimetic.

Miller WH, Alberts DP, Bhatnagar PK, Bondinell WE, Callahan JF, Calvo RR, Cousins RD, Erhard KF, Heerding DA, Keenan RM, Kwon C, Manley PJ, Newlander KA, Ross ST, Samanen JM, Uzinskas IN, Venslavsky JW, Yuan CC, Haltiwanger RC, Gowen M, Hwang SM, James IE, Lark MW, Rieman DJ, Stroup GB, Azzarano LM, Salyers KL, Smith BR, Ward KW, Johanson KO, Huffman WF.

J Med Chem. 2000 Jan 13;43(1):22-6. No abstract available.

PMID:
10633035
13.

Preclinical pharmacokinetics and interspecies scaling of a novel vitronectin receptor antagonist.

Ward KW, Azzarano LM, Bondinell WE, Cousins RD, Huffman WF, Jakas DR, Keenan RM, Ku TW, Lundberg D, Miller WH, Mumaw JA, Newlander KA, Pirhalla JL, Roethke TJ, Salyers KL, Souder PR, Stelman GJ, Smith BR.

Drug Metab Dispos. 1999 Nov;27(11):1232-41.

PMID:
10534306
14.

Design and characterization of orally active Arg-Gly-Asp peptidomimetic vitronectin receptor antagonist SB 265123 for prevention of bone loss in osteoporosis.

Lark MW, Stroup GB, Hwang SM, James IE, Rieman DJ, Drake FH, Bradbeer JN, Mathur A, Erhard KF, Newlander KA, Ross ST, Salyers KL, Smith BR, Miller WH, Huffman WF, Gowen M.

J Pharmacol Exp Ther. 1999 Nov;291(2):612-7.

PMID:
10525079
15.

Orally bioavailable nonpeptide vitronectin receptor antagonists with efficacy in an osteoporosis model.

Miller WH, Bondinell WE, Cousins RD, Erhard KF, Jakas DR, Keenan RM, Ku TW, Newlander KA, Ross ST, Haltiwanger RC, Bradbeer J, Drake FH, Gowen M, Hoffman SJ, Hwang SM, James IE, Lark MW, Lechowska B, Rieman DJ, Stroup GB, Vasko-Moser JA, Zembryki DL, Azzarano LM, Adams PC, Huffman WF, et al.

Bioorg Med Chem Lett. 1999 Jul 5;9(13):1807-12.

PMID:
10406646
16.

Conformational preferences in a benzodiazepine series of potent nonpeptide fibrinogen receptor antagonists.

Keenan RM, Callahan JF, Samanen JM, Bondinell WE, Calvo RR, Chen L, DeBrosse C, Eggleston DS, Haltiwanger RC, Hwang SM, Jakas DR, Ku TW, Miller WH, Newlander KA, Nichols A, Parker MF, Southhall LS, Uzinskas I, Vasko-Moser JA, Venslavsky JW, Wong AS, Huffman WF.

J Med Chem. 1999 Feb 25;42(4):545-59.

PMID:
10052962
17.

Hematoregulators. A case history of a novel hematoregulatory peptide, SK&F 107647.

Bhatnagar PK, Huffman WF, King AG, Løvhaug D, Pelus LM, Potts WM, Smith PL.

Pharm Biotechnol. 1998;11:367-91. Review. No abstract available.

PMID:
9760688
18.

Discovery of potent nonpeptide vitronectin receptor (alpha v beta 3) antagonists.

Keenan RM, Miller WH, Kwon C, Ali FE, Callahan JF, Calvo RR, Hwang SM, Kopple KD, Peishoff CE, Samanen JM, Wong AS, Yuan CK, Huffman WF.

J Med Chem. 1997 Jul 18;40(15):2289-92. No abstract available.

PMID:
9240343
19.

Potent, selective, orally active 3-oxo-1,4-benzodiazepine GPIIb/IIIa integrin antagonists.

Samanen JM, Ali FE, Barton LS, Bondinell WE, Burgess JL, Callahan JF, Calvo RR, Chen W, Chen L, Erhard K, Feuerstein G, Heys R, Hwang SM, Jakas DR, Keenan RM, Ku TW, Kwon C, Lee CP, Miller WH, Newlander KA, Nichols A, Parker M, Peishoff CE, Rhodes G, Ross S, Shu A, Simpson R, Takata D, Yellin TO, Uzsinskas I, Venslavsky JW, Yuan CK, Huffman WF.

J Med Chem. 1996 Dec 6;39(25):4867-70. No abstract available.

PMID:
8960544
20.

Structure-activity relationships of novel hematoregulatory peptides.

Bhatnagar PK, Agner EK, Alberts D, Arbo BE, Callahan JF, Cuthbertson AS, Engelsen SJ, Fjerdingstad H, Hartmann M, Heerding D, Hiebl J, Huffman WF, Hysben M, King AG, Kremminger P, Kwon C, LoCastro S, Løvhaug D, Pelus LM, Petteway S, Takata JS.

J Med Chem. 1996 Sep 13;39(19):3814-9.

PMID:
8809169
21.

A check on rational drug design: crystal structure of a complex of human immunodeficiency virus type 1 protease with a novel gamma-turn mimetic inhibitor.

Hoog SS, Zhao B, Winborne E, Fisher S, Green DW, DesJarlais RL, Newlander KA, Callahan JF, Moore ML, Huffman WF, et al.

J Med Chem. 1995 Aug 18;38(17):3246-52.

PMID:
7650677
22.

Potent non-peptide fibrinogen receptor antagonists which present an alternative pharmacophore.

Ku TW, Miller WH, Bondinell WE, Erhard KF, Keenan RM, Nichols AJ, Peishoff CE, Samanen JM, Wong AS, Huffman WF.

J Med Chem. 1995 Jan 6;38(1):9-12. No abstract available.

PMID:
7837245
23.

Design of a potent and orally active nonpeptide platelet fibrinogen receptor (GPIIb/IIIa) antagonist.

Bondinell WE, Keenan RM, Miller WH, Ali FE, Allen AC, de Brosse CW, Eggleston DS, Erhard KF, Haltiwanger RC, Huffman WF, et al.

Bioorg Med Chem. 1994 Sep;2(9):897-908.

PMID:
7712125
24.

A novel constrained reduced-amide inhibitor of HIV-1 protease derived from the sequential incorporation of gamma-turn mimetics into a model substrate.

Newlander KA, Callahan JF, Moore ML, Tomaszek TA Jr, Huffman WF.

J Med Chem. 1993 Aug 6;36(16):2321-31.

PMID:
8360876
25.

Antagonism of antidiuretic hormone in domestic pigs (Sus scrofa).

Monaghan ML, Divers T, Huffman WF, Kinter LB.

Gen Pharmacol. 1993 Jul;24(4):1013-20.

PMID:
8224729
26.

Anomalous antidiuretic activity of antidiuretic hormone antagonists.

Kinter LB, Caltabiano S, Huffman WF.

Biochem Pharmacol. 1993 May 5;45(9):1731-7. Review. No abstract available.

PMID:
8494530
27.

Development of GPIIb/IIIa antagonists as antithrombotic drugs.

Nichols AJ, Ruffolo RR Jr, Huffman WF, Poste G, Samanen J.

Trends Pharmacol Sci. 1992 Nov;13(11):413-7. Review.

PMID:
1440877
28.

Vasopressin antagonist inhibition of clotting factor release in the rhesus monkey (Macaca mulatta).

Kinter LB, McConnell I, Goodwin BT, Campbell S, Huffman WF, Arthus MF, Lonergan M, Bichet DG.

J Pharmacol Exp Ther. 1992 May;261(2):462-9.

PMID:
1578361
29.

Vasopressin antidiuretic agonist and antagonist activity in dogs: structural and stereochemical relationship between bridge and carboxyl terminus.

Albrightson-Winslow CR, Brickson B, Brooks DP, Bryan WM, Caldwell N, Kinter LB, Moore ML, Nambi P, Stassen FL, Huffman WF.

J Pharmacol Exp Ther. 1991 Jan;256(1):335-40.

PMID:
1988664
30.

Physiological regulation of the renal vasopressin receptor-effector pathway in dogs.

Kinter LB, Caldwell N, Caltabiano S, Winslow C, Brooks DP, Huffman WF.

Am J Physiol. 1990 Mar;258(3 Pt 2):R763-9.

PMID:
2138428
31.

Cyclooxygenase inhibition unmasks the full antidiuretic agonist activity of the vasopressin antagonist, SK&F 101926, in dogs.

Albrightson-Winslow CR, Caldwell N, Brooks DP, Huffman WF, Stassen FL, Kinter LB.

J Pharmacol Exp Ther. 1989 May;249(2):366-71.

PMID:
2524585
32.

A minor modification of residue 1 in potent vasopressin antagonists dramatically reduces agonist activity.

Huffman WF, Albrightson-Winslow C, Brickson B, Bryan HG, Caldwell N, Dytko G, Eggleston DS, Kinter LB, Moore ML, Newlander KA, et al.

J Med Chem. 1989 Apr;32(4):880-4.

PMID:
2522994
33.

Peptide substrates and inhibitors of the HIV-1 protease.

Moore ML, Bryan WM, Fakhoury SA, Magaard VW, Huffman WF, Dayton BD, Meek TD, Hyland L, Dreyer GB, Metcalf BW, et al.

Biochem Biophys Res Commun. 1989 Mar 15;159(2):420-5.

PMID:
2649094
34.

Cyclic enkephalin analogues containing alpha-amino-beta-mercapto-beta,beta-pentamethylenepropionic acid at positions 2 or 5.

Bryan WM, Callahan JF, Codd EE, Lemieux C, Moore ML, Schiller PW, Walker RF, Huffman WF.

J Med Chem. 1989 Feb;32(2):302-4.

PMID:
2536436
35.

Vasopressin receptor antagonism in rhesus monkey and man: stereochemical requirements.

Brooks DP, Koster PF, Albrightson CR, Huffman WF, Moore ML, Stassen FL, Schmidt DB, Kinter LB.

Eur J Pharmacol. 1989 Jan 24;160(1):159-62.

PMID:
2540987
36.

SK&F 105494: a potent antidiuretic hormone antagonist devoid of partial agonist activity in dogs.

Caldwell N, Brickson B, Kinter LB, Brooks DP, Huffman WF, Stassen FL, Albrightson-Winslow C.

J Pharmacol Exp Ther. 1988 Dec;247(3):897-901.

PMID:
3204522
37.

Flushing and haemodynamic responses to vasopressin peptides in the rhesus monkey.

Brooks DP, Koster PF, Stassen FL, Albrightson CR, Huffman WF, Wasserman MA, Kinter LB.

Br J Pharmacol. 1988 Jul;94(3):759-64.

38.

SK&F 105494 is a potent antidiuretic hormone antagonist in the rhesus monkey (Macaca mulatta).

Brooks DP, Koster PF, Albrightson-Winslow CR, Stassen FL, Huffman WF, Kinter LB.

J Pharmacol Exp Ther. 1988 Apr;245(1):211-5.

PMID:
3361442
39.

Design, synthesis, and biological activity of a peptide mimic of vasopressin.

Bryan WM, Hempel JC, Huffman WF, Marshall GR, Moore ML, Silvestri J, Stassen FL, Stefankiewicz JS, Sulat L, Webb RL.

J Med Chem. 1988 Apr;31(4):742-4.

PMID:
2965243
40.

Antagonists of the antidiuretic activity of vasopressin.

Kinter LB, Huffman WF, Stassen FL.

Am J Physiol. 1988 Feb;254(2 Pt 2):F165-77. Review.

PMID:
2964201
41.

Potent vasopressin antagonists modified at the carboxy-terminal tripeptide tail.

Ali FE, Chang HL, Huffman WF, Heckman G, Kinter LB, Weidley EF, Edwards R, Schmidt D, Ashton-Shue D, Stassen FL.

J Med Chem. 1987 Dec;30(12):2291-4.

PMID:
2960813
42.

Potent antagonists of vasopressin antidiuretic activity that lack the beta,beta-cyclopentamethylene-beta-mercaptopropionic acid substitution at position 1.

Yim NC, Moore ML, Huffman WF, Bryan HG, Chang HL, Kinter LB, Edwards R, Stassen FL, Schmidt D, Heckman G.

J Med Chem. 1986 Dec;29(12):2425-6. No abstract available.

PMID:
2946863
43.

Vasopressin antagonist analogs modified at position 7.

Moore ML, Greene H, Huffman WF, Stassen F, Stefankiewicz J, Sulat L, Heckman G, Schmidt D, Kinter L, McDonald J, et al.

Int J Pept Protein Res. 1986 Oct;28(4):379-85.

PMID:
2947871
44.

Syntheses and in vitro evaluation of 4-(2-aminoethyl)-2(3H)-indolones and related compounds as peripheral prejunctional dopamine receptor agonists.

DeMarinis RM, Gallagher G Jr, Hall RF, Franz RG, Webster C, Huffman WF, Schwartz MS, Kaiser C, Ross ST, Wilson JW, et al.

J Med Chem. 1986 Jun;29(6):939-47.

PMID:
3712384
45.

Potent vasopressin antagonists lacking the proline residue at position 7.

Ali FE, Bryan W, Chang HL, Huffman WF, Moore ML, Heckman G, Kinter LB, McDonald J, Schmidt D, Shue D, et al.

J Med Chem. 1986 Jun;29(6):984-8.

PMID:
2940368
46.

Novel vasopressin analogues that help define a minimum effective antagonist pharmacophore.

Huffman WF, Ali FE, Bryan WM, Callahan JF, Moore ML, Silvestri JS, Yim NC, Kinter LB, McDonald JE, Ashton-Shue D, et al.

J Med Chem. 1985 Dec;28(12):1759-60. No abstract available.

PMID:
2933517
47.

Antidiuretic hormone antagonists and aquaresis in dogs: different vasopressin sensitivity and antagonist potency in renal cortex and papilla.

Stassen FL, Heckman GD, Huffman WF, Kinter LB.

J Pharmacol Exp Ther. 1985 Jan;232(1):100-5.

PMID:
3965688
48.

Synthesis and characterization of iodinated vasopressin antagonists which retain high affinity for the vasopressin receptor.

Moore ML, Huffman WF, Roberts GD, Rottschaefer S, Sulat L, Stefankiewicz JS, Stassen F.

Biochem Biophys Res Commun. 1984 Jun 29;121(3):878-83.

PMID:
6331433
49.

4-(Aminoalkyl)-7-hydroxy-2(3H)-indolones, a novel class of potent presynaptic dopamine receptor agonists.

Huffman WF, Hall RF, Grant JA, Wilson JW, Hieble JP, Hahn RA.

J Med Chem. 1983 Jul;26(7):933-5. No abstract available.

PMID:
6306238
50.

A facile synthesis of beta-(S-benzylmercapto)-beta, beta-cyclopentamethylene-propionic acid.

Yim NC, Huffman WF.

Int J Pept Protein Res. 1983 May;21(5):568-70.

PMID:
6885243

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