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Items: 39

1.

Hit to Lead optimization of a novel class of squarate-containing polo-like kinases inhibitors.

Zhang Q, Xia Z, Mitten MJ, Lasko LM, Klinghofer V, Bouska J, Johnson EF, Penning TD, Luo Y, Giranda VL, Shoemaker AR, Stewart KD, Djuric SW, Vasudevan A.

Bioorg Med Chem Lett. 2012 Dec 15;22(24):7615-22. doi: 10.1016/j.bmcl.2012.10.009. Epub 2012 Oct 11.

PMID:
23103095
2.

Optimization of phenyl-substituted benzimidazole carboxamide poly(ADP-ribose) polymerase inhibitors: identification of (S)-2-(2-fluoro-4-(pyrrolidin-2-yl)phenyl)-1H-benzimidazole-4-carboxamide (A-966492), a highly potent and efficacious inhibitor.

Penning TD, Zhu GD, Gong J, Thomas S, Gandhi VB, Liu X, Shi Y, Klinghofer V, Johnson EF, Park CH, Fry EH, Donawho CK, Frost DJ, Buchanan FG, Bukofzer GT, Rodriguez LE, Bontcheva-Diaz V, Bouska JJ, Osterling DJ, Olson AM, Marsh KC, Luo Y, Giranda VL.

J Med Chem. 2010 Apr 22;53(8):3142-53. doi: 10.1021/jm901775y.

PMID:
20337371
3.

Discovery and SAR of substituted 3-oxoisoindoline-4-carboxamides as potent inhibitors of poly(ADP-ribose) polymerase (PARP) for the treatment of cancer.

Gandhi VB, Luo Y, Liu X, Shi Y, Klinghofer V, Johnson EF, Park C, Giranda VL, Penning TD, Zhu GD.

Bioorg Med Chem Lett. 2010 Feb 1;20(3):1023-6. doi: 10.1016/j.bmcl.2009.12.042. Epub 2009 Dec 14.

PMID:
20045315
4.

Discovery of the Poly(ADP-ribose) polymerase (PARP) inhibitor 2-[(R)-2-methylpyrrolidin-2-yl]-1H-benzimidazole-4-carboxamide (ABT-888) for the treatment of cancer.

Penning TD, Zhu GD, Gandhi VB, Gong J, Liu X, Shi Y, Klinghofer V, Johnson EF, Donawho CK, Frost DJ, Bontcheva-Diaz V, Bouska JJ, Osterling DJ, Olson AM, Marsh KC, Luo Y, Giranda VL.

J Med Chem. 2009 Jan 22;52(2):514-23. doi: 10.1021/jm801171j.

PMID:
19143569
5.

The PARP inhibitor, ABT-888 potentiates temozolomide: correlation with drug levels and reduction in PARP activity in vivo.

Palma JP, Rodriguez LE, Bontcheva-Diaz VD, Bouska JJ, Bukofzer G, Colon-Lopez M, Guan R, Jarvis K, Johnson EF, Klinghofer V, Liu X, Olson A, Saltarelli MJ, Shi Y, Stavropoulos JA, Zhu GD, Penning TD, Luo Y, Giranda VL, Rosenberg SH, Frost DJ, Donawho CK.

Anticancer Res. 2008 Sep-Oct;28(5A):2625-35.

6.

Potentiation of temozolomide cytotoxicity by poly(ADP)ribose polymerase inhibitor ABT-888 requires a conversion of single-stranded DNA damages to double-stranded DNA breaks.

Liu X, Shi Y, Guan R, Donawho C, Luo Y, Palma J, Zhu GD, Johnson EF, Rodriguez LE, Ghoreishi-Haack N, Jarvis K, Hradil VP, Colon-Lopez M, Cox BF, Klinghofer V, Penning T, Rosenberg SH, Frost D, Giranda VL, Luo Y.

Mol Cancer Res. 2008 Oct;6(10):1621-9. doi: 10.1158/1541-7786.MCR-08-0240.

7.

Isoxazolo[3,4-b]quinoline-3,4(1H,9H)-diones as unique, potent and selective inhibitors for Pim-1 and Pim-2 kinases: chemistry, biological activities, and molecular modeling.

Tong Y, Stewart KD, Thomas S, Przytulinska M, Johnson EF, Klinghofer V, Leverson J, McCall O, Soni NB, Luo Y, Lin NH, Sowin TJ, Giranda VL, Penning TD.

Bioorg Med Chem Lett. 2008 Oct 1;18(19):5206-8. doi: 10.1016/j.bmcl.2008.08.079. Epub 2008 Aug 28.

PMID:
18790640
8.

Synthesis and SAR of novel, potent and orally bioavailable benzimidazole inhibitors of poly(ADP-ribose) polymerase (PARP) with a quaternary methylene-amino substituent.

Zhu GD, Gandhi VB, Gong J, Thomas S, Luo Y, Liu X, Shi Y, Klinghofer V, Johnson EF, Frost D, Donawho C, Jarvis K, Bouska J, Marsh KC, Rosenberg SH, Giranda VL, Penning TD.

Bioorg Med Chem Lett. 2008 Jul 15;18(14):3955-8. doi: 10.1016/j.bmcl.2008.06.023. Epub 2008 Jun 12.

PMID:
18586490
9.

Discovery and SAR of 2-(1-propylpiperidin-4-yl)-1H-benzimidazole-4-carboxamide: A potent inhibitor of poly(ADP-ribose) polymerase (PARP) for the treatment of cancer.

Penning TD, Zhu GD, Gandhi VB, Gong J, Thomas S, Lubisch W, Grandel R, Wernet W, Park CH, Fry EH, Liu X, Shi Y, Klinghofer V, Johnson EF, Donawho CK, Frost DJ, Bontcheva-Diaz V, Bouska JJ, Olson AM, Marsh KC, Luo Y, Rosenberg SH, Giranda VL.

Bioorg Med Chem. 2008 Jul 15;16(14):6965-75. doi: 10.1016/j.bmc.2008.05.044. Epub 2008 May 27.

PMID:
18541433
10.

Syntheses of potent, selective, and orally bioavailable indazole-pyridine series of protein kinase B/Akt inhibitors with reduced hypotension.

Zhu GD, Gandhi VB, Gong J, Thomas S, Woods KW, Song X, Li T, Diebold RB, Luo Y, Liu X, Guan R, Klinghofer V, Johnson EF, Bouska J, Olson A, Marsh KC, Stoll VS, Mamo M, Polakowski J, Campbell TJ, Martin RL, Gintant GA, Penning TD, Li Q, Rosenberg SH, Giranda VL.

J Med Chem. 2007 Jun 28;50(13):2990-3003. Epub 2007 May 25.

PMID:
17523610
11.

ABT-888, an orally active poly(ADP-ribose) polymerase inhibitor that potentiates DNA-damaging agents in preclinical tumor models.

Donawho CK, Luo Y, Luo Y, Penning TD, Bauch JL, Bouska JJ, Bontcheva-Diaz VD, Cox BF, DeWeese TL, Dillehay LE, Ferguson DC, Ghoreishi-Haack NS, Grimm DR, Guan R, Han EK, Holley-Shanks RR, Hristov B, Idler KB, Jarvis K, Johnson EF, Kleinberg LR, Klinghofer V, Lasko LM, Liu X, Marsh KC, McGonigal TP, Meulbroek JA, Olson AM, Palma JP, Rodriguez LE, Shi Y, Stavropoulos JA, Tsurutani AC, Zhu GD, Rosenberg SH, Giranda VL, Frost DJ.

Clin Cancer Res. 2007 May 1;13(9):2728-37.

12.

Design and synthesis of pyridine-pyrazolopyridine-based inhibitors of protein kinase B/Akt.

Zhu GD, Gong J, Gandhi VB, Woods K, Luo Y, Liu X, Guan R, Klinghofer V, Johnson EF, Stoll VS, Mamo M, Li Q, Rosenberg SH, Giranda VL.

Bioorg Med Chem. 2007 Mar 15;15(6):2441-52. Epub 2007 Jan 17.

PMID:
17258463
13.

Synthesis and SAR of indazole-pyridine based protein kinase B/Akt inhibitors.

Woods KW, Fischer JP, Claiborne A, Li T, Thomas SA, Zhu GD, Diebold RB, Liu X, Shi Y, Klinghofer V, Han EK, Guan R, Magnone SR, Johnson EF, Bouska JJ, Olson AM, de Jong R, Oltersdorf T, Luo Y, Rosenberg SH, Giranda VL, Li Q.

Bioorg Med Chem. 2006 Oct 15;14(20):6832-46. Epub 2006 Jul 14.

PMID:
16843670
14.

Identification of a novel 3,5-disubstituted pyridine as a potent, selective, and orally active inhibitor of Akt1 kinase.

Thomas SA, Li T, Woods KW, Song X, Packard G, Fischer JP, Diebold RB, Liu X, Shi Y, Klinghofer V, Johnson EF, Bouska JJ, Olson A, Guan R, Magnone SR, Marsh K, Luo Y, Rosenberg SH, Giranda VL, Li Q.

Bioorg Med Chem Lett. 2006 Jul 15;16(14):3740-4. Epub 2006 May 5.

PMID:
16678413
15.

Discovery and SAR of oxindole-pyridine-based protein kinase B/Akt inhibitors for treating cancers.

Zhu GD, Gandhi VB, Gong J, Luo Y, Liu X, Shi Y, Guan R, Magnone SR, Klinghofer V, Johnson EF, Bouska J, Shoemaker A, Oleksijew A, Jarvis K, Park C, Jong RD, Oltersdorf T, Li Q, Rosenberg SH, Giranda VL.

Bioorg Med Chem Lett. 2006 Jul 1;16(13):3424-9. Epub 2006 Apr 27.

PMID:
16644221
16.

Isoquinoline-pyridine-based protein kinase B/Akt antagonists: SAR and in vivo antitumor activity.

Zhu GD, Gong J, Claiborne A, Woods KW, Gandhi VB, Thomas S, Luo Y, Liu X, Shi Y, Guan R, Magnone SR, Klinghofer V, Johnson EF, Bouska J, Shoemaker A, Oleksijew A, Stoll VS, De Jong R, Oltersdorf T, Li Q, Rosenberg SH, Giranda VL.

Bioorg Med Chem Lett. 2006 Jun 15;16(12):3150-5. Epub 2006 Apr 5.

PMID:
16603355
17.

Synthesis and structure-activity relationship of 3,4'-bispyridinylethylenes: discovery of a potent 3-isoquinolinylpyridine inhibitor of protein kinase B (PKB/Akt) for the treatment of cancer.

Li Q, Woods KW, Thomas S, Zhu GD, Packard G, Fisher J, Li T, Gong J, Dinges J, Song X, Abrams J, Luo Y, Johnson EF, Shi Y, Liu X, Klinghofer V, Des Jong R, Oltersdorf T, Stoll VS, Jakob CG, Rosenberg SH, Giranda VL.

Bioorg Med Chem Lett. 2006 Apr 1;16(7):2000-7. Epub 2006 Jan 18.

PMID:
16413780
18.

Discovery of trans-3,4'-bispyridinylethylenes as potent and novel inhibitors of protein kinase B (PKB/Akt) for the treatment of cancer: Synthesis and biological evaluation.

Li Q, Li T, Zhu GD, Gong J, Claibone A, Dalton C, Luo Y, Johnson EF, Shi Y, Liu X, Klinghofer V, Bauch JL, Marsh KC, Bouska JJ, Arries S, De Jong R, Oltersdorf T, Stoll VS, Jakob CG, Rosenberg SH, Giranda VL.

Bioorg Med Chem Lett. 2006 Mar 15;16(6):1679-85. Epub 2006 Jan 5.

PMID:
16403626
19.

Optimal classes of chemotherapeutic agents sensitized by specific small-molecule inhibitors of akt in vitro and in vivo.

Shi Y, Liu X, Han EK, Guan R, Shoemaker AR, Oleksijew A, Woods KW, Fisher JP, Klinghofer V, Lasko L, McGonigal T, Li Q, Rosenberg SH, Giranda VL, Luo Y.

Neoplasia. 2005 Nov;7(11):992-1000.

20.

Potent and selective inhibitors of Akt kinases slow the progress of tumors in vivo.

Luo Y, Shoemaker AR, Liu X, Woods KW, Thomas SA, de Jong R, Han EK, Li T, Stoll VS, Powlas JA, Oleksijew A, Mitten MJ, Shi Y, Guan R, McGonigal TP, Klinghofer V, Johnson EF, Leverson JD, Bouska JJ, Mamo M, Smith RA, Gramling-Evans EE, Zinker BA, Mika AK, Nguyen PT, Oltersdorf T, Rosenberg SH, Li Q, Giranda VL.

Mol Cancer Ther. 2005 Jun;4(6):977-86.

21.

Naphthamidine urokinase plasminogen activator inhibitors with improved pharmacokinetic properties.

Bruncko M, McClellan WJ, Wendt MD, Sauer DR, Geyer A, Dalton CR, Kaminski MA, Weitzberg M, Gong J, Dellaria JF, Mantei R, Zhao X, Nienaber VL, Stewart K, Klinghofer V, Bouska J, Rockway TW, Giranda VL.

Bioorg Med Chem Lett. 2005 Jan 3;15(1):93-8.

PMID:
15582418
22.

Interaction with the S1 beta-pocket of urokinase: 8-heterocycle substituted and 6,8-disubstituted 2-naphthamidine urokinase inhibitors.

Wendt MD, Geyer A, McClellan WJ, Rockway TW, Weitzberg M, Zhao X, Mantei R, Stewart K, Nienaber V, Klinghofer V, Giranda VL.

Bioorg Med Chem Lett. 2004 Jun 21;14(12):3063-8.

PMID:
15149645
23.

Pseudosubstrate peptides inhibit Akt and induce cell growth inhibition.

Luo Y, Smith RA, Guan R, Liu X, Klinghofer V, Shen J, Hutchins C, Richardson P, Holzman T, Rosenberg SH, Giranda VL.

Biochemistry. 2004 Feb 10;43(5):1254-63.

PMID:
14756561
24.

Identification of novel binding interactions in the development of potent, selective 2-naphthamidine inhibitors of urokinase. Synthesis, structural analysis, and SAR of N-phenyl amide 6-substitution.

Wendt MD, Rockway TW, Geyer A, McClellan W, Weitzberg M, Zhao X, Mantei R, Nienaber VL, Stewart K, Klinghofer V, Giranda VL.

J Med Chem. 2004 Jan 15;47(2):303-24.

PMID:
14711304
25.

Species specificity of amidine-based urokinase inhibitors.

Klinghofer V, Stewart K, McGonigal T, Smith R, Sarthy A, Nienaber V, Butler C, Dorwin S, Richardson P, Weitzberg M, Wendt M, Rockway T, Zhao X, Hulkower KI, Giranda VL.

Biochemistry. 2001 Aug 7;40(31):9125-31.

PMID:
11478879
26.

Structure-directed discovery of potent non-peptidic inhibitors of human urokinase that access a novel binding subsite.

Nienaber VL, Davidson D, Edalji R, Giranda VL, Klinghofer V, Henkin J, Magdalinos P, Mantei R, Merrick S, Severin JM, Smith RA, Stewart K, Walter K, Wang J, Wendt M, Weitzberg M, Zhao X, Rockway T.

Structure. 2000 May 15;8(5):553-63.

27.

Discovery of a new cyclooxygenase-2 lead compound through 3-D database searching and combinatorial chemistry.

Stewart KD, Loren S, Frey L, Otis E, Klinghofer V, Hulkower KI.

Bioorg Med Chem Lett. 1998 Mar 3;8(5):529-34.

PMID:
9871612
28.

The nitric oxide synthase inhibitor, L-NG-monomethylarginine, reduces carrageenan-induced pleurisy in the rat.

Tracey WR, Nakane M, Kuk J, Budzik G, Klinghofer V, Harris R, Carter G.

J Pharmacol Exp Ther. 1995 Jun;273(3):1295-9.

PMID:
7540689
29.

Novel potent and selective inhibitors of inducible nitric oxide synthase.

Nakane M, Klinghofer V, Kuk JE, Donnelly JL, Budzik GP, Pollock JS, Basha F, Carter GW.

Mol Pharmacol. 1995 Apr;47(4):831-4.

PMID:
7536889
30.

Functional expression of three isoforms of human nitric oxide synthase in baculovirus-infected insect cells.

Nakane M, Pollock JS, Klinghofer V, Basha F, Marsden PA, Hokari A, Ogura T, Esumi H, Carter GW.

Biochem Biophys Res Commun. 1995 Jan 17;206(2):511-7.

PMID:
7530001
31.

Nonpeptide renin inhibitors with good intraduodenal bioavailability and efficacy in dog.

Boyd SA, Fung AK, Baker WR, Mantei RA, Stein HH, Cohen J, Barlow JL, Klinghofer V, Wessale JL, Verburg KM, et al.

J Med Chem. 1994 Sep 16;37(19):2991-3007.

PMID:
7932521
32.

Immunochemical detection of inducible NO synthase in human lung.

Tracey WR, Xue C, Klinghofer V, Barlow J, Pollock JS, Förstermann U, Johns RA.

Am J Physiol. 1994 Jun;266(6 Pt 1):L722-7.

PMID:
7517641
33.

Cardiovascular effects and hemodynamic mechanism of action of the novel, nonpeptidic renin inhibitor A-74273 in dogs.

Wessale JL, Calzadilla SV, Boyd SA, Baker WR, Stein HH, Kovar PJ, Barlow J, Klinghofer V, Mantei R, Kleinert HD.

J Cardiovasc Pharmacol. 1993 Oct;22(4):644-52.

PMID:
7505369
35.

Effects of high doses of A-74273, a novel nonpeptidic and orally bioavailable renin inhibitor.

Verburg KM, Polakowski JS, Kovar PJ, Klinghofer V, Barlow JL, Stein HH, Mantei RA, Fung AK, Boyd SA, Baker WR, et al.

J Cardiovasc Pharmacol. 1993 Jan;21(1):149-55.

PMID:
7678671
36.

Discovery of a peptide-based renin inhibitor with oral bioavailability and efficacy.

Kleinert HD, Rosenberg SH, Baker WR, Stein HH, Klinghofer V, Barlow J, Spina K, Polakowski J, Kovar P, Cohen J, et al.

Science. 1992 Sep 25;257(5078):1940-3.

PMID:
1411510
37.

Endothelial nitric oxide synthase is myristylated.

Pollock JS, Klinghofer V, Förstermann U, Murad F.

FEBS Lett. 1992 Sep 14;309(3):402-4.

38.

C-terminal modifications of nonpeptide renin inhibitors: improved oral bioavailability via modification of physicochemical properties.

Boyd SA, Fung AK, Baker WR, Mantei RA, Armiger YL, Stein HH, Cohen J, Egan DA, Barlow JL, Klinghofer V, et al.

J Med Chem. 1992 May 15;35(10):1735-46.

PMID:
1588555
39.

Directly photocrosslinked nucleotides joining transfer RNA to aminoacyl-tRNA synthetase in methionine and tyrosine systems.

Ackerman EJ, Joachimiak A, Klinghofer V, Sigler PB.

J Mol Biol. 1985 Jan 5;181(1):93-102.

PMID:
2580097

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