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Items: 44

1.

Discovery and optimization of a highly efficacious class of 5-aryl-2-aminopyridines as FMS-like tyrosine kinase 3 (FLT3) inhibitors.

Liu G, Abraham S, Liu X, Xu S, Rooks AM, Nepomuceno R, Dao A, Brigham D, Gitnick D, Insko DE, Gardner MF, Zarrinkar PP, Christopher R, Belli B, Armstrong RC, Holladay MW.

Bioorg Med Chem Lett. 2015 Sep 1;25(17):3436-41. doi: 10.1016/j.bmcl.2015.07.023. Epub 2015 Jul 14.

PMID:
26208887
2.

Discovery of AC710, a Globally Selective Inhibitor of Platelet-Derived Growth Factor Receptor-Family Kinases.

Liu G, Campbell BT, Holladay MW, Ford Pulido JM, Hua H, Gitnick D, Gardner MF, James J, Breider MA, Brigham D, Belli B, Armstrong RC, Treiber DK.

ACS Med Chem Lett. 2012 Sep 24;3(12):997-1002. doi: 10.1021/ml300214g. eCollection 2012 Dec 13.

3.

Discovery of highly potent and selective pan-Aurora kinase inhibitors with enhanced in vivo antitumor therapeutic index.

Liu G, Abraham S, Tran L, Vickers TD, Xu S, Hadd MJ, Quiambao S, Holladay MW, Hua H, Ford Pulido JM, Gunawardane RN, Davis MI, Eichelberger SR, Apuy JL, Gitnick D, Gardner MF, James J, Breider MA, Belli B, Armstrong RC, Treiber DK.

J Med Chem. 2012 Apr 12;55(7):3250-60. doi: 10.1021/jm201702g. Epub 2012 Mar 14.

PMID:
22380736
4.

CEP-32496: a novel orally active BRAF(V600E) inhibitor with selective cellular and in vivo antitumor activity.

James J, Ruggeri B, Armstrong RC, Rowbottom MW, Jones-Bolin S, Gunawardane RN, Dobrzanski P, Gardner MF, Zhao H, Cramer MD, Hunter K, Nepomuceno RR, Cheng M, Gitnick D, Yazdanian M, Insko DE, Ator MA, Apuy JL, Faraoni R, Dorsey BD, Williams M, Bhagwat SS, Holladay MW.

Mol Cancer Ther. 2012 Apr;11(4):930-41. doi: 10.1158/1535-7163.MCT-11-0645. Epub 2012 Feb 7.

5.

Identification of 1-(3-(6,7-dimethoxyquinazolin-4-yloxy)phenyl)-3-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)urea hydrochloride (CEP-32496), a highly potent and orally efficacious inhibitor of V-RAF murine sarcoma viral oncogene homologue B1 (BRAF) V600E.

Rowbottom MW, Faraoni R, Chao Q, Campbell BT, Lai AG, Setti E, Ezawa M, Sprankle KG, Abraham S, Tran L, Struss B, Gibney M, Armstrong RC, Gunawardane RN, Nepomuceno RR, Valenta I, Hua H, Gardner MF, Cramer MD, Gitnick D, Insko DE, Apuy JL, Jones-Bolin S, Ghose AK, Herbertz T, Ator MA, Dorsey BD, Ruggeri B, Williams M, Bhagwat S, James J, Holladay MW.

J Med Chem. 2012 Feb 9;55(3):1082-105. doi: 10.1021/jm2009925. Epub 2012 Jan 23.

PMID:
22168626
6.

4-Quinazolinyloxy-diaryl ureas as novel BRAFV600E inhibitors.

Holladay MW, Campbell BT, Rowbottom MW, Chao Q, Sprankle KG, Lai AG, Abraham S, Setti E, Faraoni R, Tran L, Armstrong RC, Gunawardane RN, Gardner MF, Cramer MD, Gitnick D, Ator MA, Dorsey BD, Ruggeri BR, Williams M, Bhagwat SS, James J.

Bioorg Med Chem Lett. 2011 Sep 15;21(18):5342-6. doi: 10.1016/j.bmcl.2011.07.019. Epub 2011 Jul 14.

PMID:
21807507
7.

Novel series of pyrrolotriazine analogs as highly potent pan-Aurora kinase inhibitors.

Abraham S, Hadd MJ, Tran L, Vickers T, Sindac J, Milanov ZV, Holladay MW, Bhagwat SS, Hua H, Ford Pulido JM, Cramer MD, Gitnick D, James J, Dao A, Belli B, Armstrong RC, Treiber DK, Liu G.

Bioorg Med Chem Lett. 2011 Sep 15;21(18):5296-300. doi: 10.1016/j.bmcl.2011.07.027. Epub 2011 Jul 14.

PMID:
21802948
8.

Synthesis and structure-activity studies on N-[5-(1H-imidazol-4-yl)-5,6,7,8-tetrahydro-1-naphthalenyl]methanesulfonamide, an imidazole-containing alpha(1A)-adrenoceptor agonist.

Altenbach RJ, Khilevich A, Kolasa T, Rohde JJ, Bhatia PA, Patel MV, Searle XB, Yang F, Bunnelle WH, Tietje K, Bayburt EK, Carroll WA, Meyer MD, Henry R, Buckner SA, Kuk J, Daza AV, Milicic IV, Cain JC, Kang CH, Ireland LM, Carr TL, Miller TR, Hancock AA, Nakane M, Esbenshade TA, Brune ME, O'Neill AB, Gauvin DM, Katwala SP, Holladay MW, Brioni JD, Sullivan JP.

J Med Chem. 2004 Jun 3;47(12):3220-35.

PMID:
15163201
9.

Synthesis and structure-activity relationships of a novel series of 2,3,5,6,7,9-hexahydrothieno[3,2-b]quinolin-8(4H)-one 1,1-dioxide K(ATP) channel openers: discovery of (-)-(9S)-9-(3-bromo-4-fluorophenyl)-2,3,5,6,7,9- hexahydrothieno[3,2-b]quinolin-8(4H)-one 1,1-dioxide (A-278637), a potent K(ATP) opener that selectively inhibits spontaneous bladder contractions.

Carroll WA, Altenbach RJ, Bai H, Brioni JD, Brune ME, Buckner SA, Cassidy C, Chen Y, Coghlan MJ, Daza AV, Drizin I, Fey TA, Fitzgerald M, Gopalakrishnan M, Gregg RJ, Henry RF, Holladay MW, King LL, Kort ME, Kym PR, Milicic I, Tang R, Turner SC, Whiteaker KL, Yi L, Zhang H, Sullivan JP.

J Med Chem. 2004 Jun 3;47(12):3163-79.

PMID:
15163196
10.

N-[3-(1H-imidazol-4-ylmethyl)phenyl]ethanesulfonamide (ABT-866, 1),(1) a novel alpha(1)-adrenoceptor ligand with an enhanced in vitro and in vivo profile relative to phenylpropanolamine and midodrine.

Altenbach RJ, Khilevich A, Meyer MD, Buckner SA, Milicic I, Daza AV, Brune ME, O'Neill AB, Gauvin DM, Cain JC, Nakane M, Holladay MW, Williams M, Brioni JD, Sullivan JP.

J Med Chem. 2002 Sep 26;45(20):4395-7.

PMID:
12238918
11.

Structure-Activity studies for a novel series of tricyclic dihydropyrimidines as K(ATP) channel openers (KCOs).

Drizin I, Holladay MW, Yi L, Zhang HQ, Gopalakrishnan S, Gopalakrishnan M, Whiteaker KL, Buckner SA, Sullivan JP, Carroll WA.

Bioorg Med Chem Lett. 2002 Jun 3;12(11):1481-4.

PMID:
12031324
12.

Solid phase heterocyclic chemistry.

Krchnák V, Holladay MW.

Chem Rev. 2002 Jan;102(1):61-91. No abstract available.

PMID:
11782129
13.

Synthesis and structure-activity relationships of 5-substituted pyridine analogues of 3.

Lin NH, Li Y, He Y, Holladay MW, Kuntzweiler T, Anderson DJ, Campbell JE, Arneric SP.

Bioorg Med Chem Lett. 2001 Mar 12;11(5):631-3.

PMID:
11266158
15.

Structure-activity studies related to ABT-594, a potent nonopioid analgesic agent: effect of pyridine and azetidine ring substitutions on nicotinic acetylcholine receptor binding affinity and analgesic activity in mice.

Holladay MW, Bai H, Li Y, Lin NH, Daanen JF, Ryther KB, Wasicak JT, Kincaid JF, He Y, Hettinger AM, Huang P, Anderson DJ, Bannon AW, Buckley MJ, Campbell JE, Donnelly-Roberts DL, Gunther KL, Kim DJ, Kuntzweiler TA, Sullivan JP, Decker MW, Arneric SP.

Bioorg Med Chem Lett. 1998 Oct 6;8(19):2797-802.

PMID:
9873625
16.

Synthesis and structure-activity relationships of pyridine-modified analogs of 3-[2-((S)-pyrrolidinyl)methoxy]pyridine, A-84543, a potent nicotinic acetylcholine receptor agonist.

Lin NH, Gunn DE, Li Y, He Y, Bai H, Ryther KB, Kuntzweiler T, Donnelly-Roberts DL, Anderson DJ, Campbell JE, Sullivan JP, Arneric SP, Holladay MW.

Bioorg Med Chem Lett. 1998 Feb 3;8(3):249-54.

PMID:
9871663
17.

The role of neuronal nicotinic acetylcholine receptors in antinociception: effects of ABT-594.

Decker MW, Curzon P, Holladay MW, Nikkel AL, Bitner RS, Bannon AW, Donnelly-Roberts DL, Puttfarcken PS, Kuntzweiler TA, Briggs CA, Williams M, Arneric SP.

J Physiol Paris. 1998 Jun-Aug;92(3-4):221-4. Review.

PMID:
9789812
18.

Antinociceptive effects of the novel neuronal nicotinic acetylcholine receptor agonist, ABT-594, in mice.

Decker MW, Bannon AW, Buckley MJ, Kim DJ, Holladay MW, Ryther KB, Lin NH, Wasicak JT, Williams M, Arneric SP.

Eur J Pharmacol. 1998 Apr 3;346(1):23-33.

PMID:
9617748
19.

ABT-594 [(R)-5-(2-azetidinylmethoxy)-2-chloropyridine]: a novel, orally effective antinociceptive agent acting via neuronal nicotinic acetylcholine receptors: II. In vivo characterization.

Bannon AW, Decker MW, Curzon P, Buckley MJ, Kim DJ, Radek RJ, Lynch JK, Wasicak JT, Lin NH, Arnold WH, Holladay MW, Williams M, Arneric SP.

J Pharmacol Exp Ther. 1998 May;285(2):787-94.

PMID:
9580627
20.

ABT-594 [(R)-5-(2-azetidinylmethoxy)-2-chloropyridine]: a novel, orally effective analgesic acting via neuronal nicotinic acetylcholine receptors: I. In vitro characterization.

Donnelly-Roberts DL, Puttfarcken PS, Kuntzweiler TA, Briggs CA, Anderson DJ, Campbell JE, Piattoni-Kaplan M, McKenna DG, Wasicak JT, Holladay MW, Williams M, Arneric SP.

J Pharmacol Exp Ther. 1998 May;285(2):777-86.

PMID:
9580626
21.

Identification and initial structure-activity relationships of (R)-5-(2-azetidinylmethoxy)-2-chloropyridine (ABT-594), a potent, orally active, non-opiate analgesic agent acting via neuronal nicotinic acetylcholine receptors.

Holladay MW, Wasicak JT, Lin NH, He Y, Ryther KB, Bannon AW, Buckley MJ, Kim DJ, Decker MW, Anderson DJ, Campbell JE, Kuntzweiler TA, Donnelly-Roberts DL, Piattoni-Kaplan M, Briggs CA, Williams M, Arneric SP.

J Med Chem. 1998 Feb 12;41(4):407-12.

PMID:
9484491
22.

Broad-spectrum, non-opioid analgesic activity by selective modulation of neuronal nicotinic acetylcholine receptors.

Bannon AW, Decker MW, Holladay MW, Curzon P, Donnelly-Roberts D, Puttfarcken PS, Bitner RS, Diaz A, Dickenson AH, Porsolt RD, Williams M, Arneric SP.

Science. 1998 Jan 2;279(5347):77-81.

23.

Neuronal nicotinic acetylcholine receptors as targets for drug discovery.

Holladay MW, Dart MJ, Lynch JK.

J Med Chem. 1997 Dec 19;40(26):4169-94. Review. No abstract available.

PMID:
9435889
24.

ABT-089 [2-methyl-3-(2-(S)-pyrrolidinylmethoxy)pyridine dihydrochloride]: II. A novel cholinergic channel modulator with effects on cognitive performance in rats and monkeys.

Decker MW, Bannon AW, Curzon P, Gunther KL, Brioni JD, Holladay MW, Lin NH, Li Y, Daanen JF, Buccafusco JJ, Prendergast MA, Jackson WJ, Arneric SP.

J Pharmacol Exp Ther. 1997 Oct;283(1):247-58.

PMID:
9336330
25.

ABT-089 [2-methyl-3-(2-(S)-pyrrolidinylmethoxy)pyridine]: I. A potent and selective cholinergic channel modulator with neuroprotective properties.

Sullivan JP, Donnelly-Roberts D, Briggs CA, Anderson DJ, Gopalakrishnan M, Xue IC, Piattoni-Kaplan M, Molinari E, Campbell JE, McKenna DG, Gunn DE, Lin NH, Ryther KB, He Y, Holladay MW, Wonnacott S, Williams M, Arneric SP.

J Pharmacol Exp Ther. 1997 Oct;283(1):235-46.

PMID:
9336329
26.

Functional characterization of the novel neuronal nicotinic acetylcholine receptor ligand GTS-21 in vitro and in vivo.

Briggs CA, Anderson DJ, Brioni JD, Buccafusco JJ, Buckley MJ, Campbell JE, Decker MW, Donnelly-Roberts D, Elliott RL, Gopalakrishnan M, Holladay MW, Hui YH, Jackson WJ, Kim DJ, Marsh KC, O'Neill A, Prendergast MA, Ryther KB, Sullivan JP, Arneric SP.

Pharmacol Biochem Behav. 1997 May-Jun;57(1-2):231-41.

PMID:
9164577
27.

Structure-activity studies on 2-methyl-3-(2(S)-pyrrolidinylmethoxy) pyridine (ABT-089): an orally bioavailable 3-pyridyl ether nicotinic acetylcholine receptor ligand with cognition-enhancing properties.

Lin NH, Gunn DE, Ryther KB, Garvey DS, Donnelly-Roberts DL, Decker MW, Brioni JD, Buckley MJ, Rodrigues AD, Marsh KG, Anderson DJ, Buccafusco JJ, Prendergast MA, Sullivan JP, Williams M, Arneric SP, Holladay MW.

J Med Chem. 1997 Jan 31;40(3):385-90.

PMID:
9022806
28.

Lycaconitine revisited: partial synthesis and neuronal nicotinic acetylcholine receptor affinities.

Jacyno JM, Harwood JS, Lin NH, Campbell JE, Sullivan JP, Holladay MW.

J Nat Prod. 1996 Jul;59(7):707-9.

PMID:
8759171
29.

A-85380 [3-(2(S)-azetidinylmethoxy) pyridine]: in vitro pharmacological properties of a novel, high affinity alpha 4 beta 2 nicotinic acetylcholine receptor ligand.

Sullivan JP, Donnelly-Roberts D, Briggs CA, Anderson DJ, Gopalakrishnan M, Piattoni-Kaplan M, Campbell JE, McKenna DG, Molinari E, Hettinger AM, Garvey DS, Wasicak JT, Holladay MW, Williams M, Arneric SP.

Neuropharmacology. 1996 Jun;35(6):725-34.

PMID:
8887981
30.

Novel 3-Pyridyl ethers with subnanomolar affinity for central neuronal nicotinic acetylcholine receptors.

Abreo MA, Lin NH, Garvey DS, Gunn DE, Hettinger AM, Wasicak JT, Pavlik PA, Martin YC, Donnelly-roberts DL, Anderson DJ, Sullivan JP, Williams M, Arneric SP, Holladay MW.

J Med Chem. 1996 Feb 16;39(4):817-25.

PMID:
8632405
31.

Cholinergic channel activators: novel opportunities for the treatment of CNS disorders.

Sullivan JP, Decker MW, Donnelly-Roberts D, Brioni JD, Bannon AW, Holladay MW, Anderson DJ, Briggs CA, Williams M, Arneric SP.

Proc West Pharmacol Soc. 1995;38:127-30. Review.

PMID:
7480004
32.

Ligands for brain cholinergic channel receptors: synthesis and in vitro characterization of novel isoxazoles and isothiazoles as bioisosteric replacements for the pyridine ring in nicotine.

Garvey DS, Wasicak JT, Elliott RL, Lebold SA, Hettinger AM, Carrera GM, Lin NH, He Y, Holladay MW, Anderson DJ, et al.

J Med Chem. 1994 Dec 23;37(26):4455-63.

PMID:
7799396
33.

Novel isoxazoles which interact with brain cholinergic channel receptors have intrinsic cognitive enhancing and anxiolytic activities.

Garvey DS, Wasicak JT, Decker MW, Brioni JD, Buckley MJ, Sullivan JP, Carrera GM, Holladay MW, Arneric SP, Williams M.

J Med Chem. 1994 Apr 15;37(8):1055-9. No abstract available.

PMID:
7909335
34.

Tetrapeptide CCK-A agonists: effect of backbone N-methylations on in vitro and in vivo CCK activity.

Holladay MW, Kopecka H, Miller TR, Bednarz L, Nikkel AL, Bianchi BR, Witte DG, Shiosaki K, Lin CW, Asin KE, et al.

J Med Chem. 1994 Mar 4;37(5):630-5.

PMID:
8126703
35.

Double bond isosteres of the peptide bond: synthesis and biological activity of cholecystokinin (CCK) C-terminal hexapeptide analogs.

Shue YK, Tufano MD, Carrera GM Jr, Kopecka H, Kuyper SL, Holladay MW, Lin CW, Witte DG, Miller TR, Stashko M, et al.

Bioorg Med Chem. 1993 Sep;1(3):161-71.

PMID:
8081848
36.

Synthesis and biological activity of CCK heptapeptide analogues. Effects of conformational constraints and standard modifications on receptor subtype selectivity, functional activity in vitro, and appetite suppression in vivo.

Holladay MW, Bennett MJ, Tufano MD, Lin CW, Asin KE, Witte DG, Miller TR, Bianchi BR, Nikkel AL, Bednarz L, et al.

J Med Chem. 1992 Aug 7;35(16):2919-28.

PMID:
1501220
38.

A71378: a CCK agonist with high potency and selectivity for CCK-A receptors.

Lin CW, Holladay MW, Witte DG, Miller TR, Wolfram CA, Bianchi BR, Bennett MJ, Nadzan AM.

Am J Physiol. 1990 Apr;258(4 Pt 1):G648-51.

PMID:
2333977
39.

Distinct requirements for activation at CCK-A and CCK-B/gastrin receptors: studies with a C-terminal hydrazide analogue of cholecystokinin tetrapeptide (30-33).

Lin CW, Holladay MW, Barrett RW, Wolfram CA, Miller TR, Witte D, Kerwin JF Jr, Wagenaar F, Nadzan AM.

Mol Pharmacol. 1989 Dec;36(6):881-6.

PMID:
2601685
40.
41.

Pepsin-catalysed addition of water to a ketomethylene peptide isostere: observation of the tetrahedral species by 13C-nuclear-magnetic-resonance spectroscopy.

Holladay MW, Salituro FG, Schmidt PG, Rich DH.

Biochem Soc Trans. 1985 Dec;13(6):1046-8. No abstract available.

PMID:
3937753
42.
43.

Gentisuric acid: metabolic formation in animals and identification as a metabolite of aspirin in man.

Wilson JT, Howell RL, Holladay MW, Brilis GM, Chrastil J, Watson JT, Taber DF.

Clin Pharmacol Ther. 1978 Jun;23(6):635-43.

PMID:
417892
44.

Biologically oriented organic sulfur chemistry. 15. Organic disulfides and related substances. 41. Inhibition of the fungal pathogen Histoplasma capsulatum by some organic disulfides.

Field L, Grimaldi JA Jr, Hanley WS, Holladay MW, Ravichandran R, Schaad LJ, Tate CE.

J Med Chem. 1977 Aug;20(8):996-1001.

PMID:
330858

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