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Items: 38

1.

Pyrimidine-based tricyclic molecules as potent and orally efficacious inhibitors of wee1 kinase.

Tong Y, Torrent M, Florjancic AS, Bromberg KD, Buchanan FG, Ferguson DC, Johnson EF, Lasko LM, Maag D, Merta PJ, Olson AM, Osterling DJ, Soni N, Shoemaker AR, Penning TD.

ACS Med Chem Lett. 2014 Aug 6;6(1):58-62. doi: 10.1021/ml5002745. eCollection 2015 Jan 8.

2.

Azaindole-Based Inhibitors of Cdc7 Kinase: Impact of the Pre-DFG Residue, Val 195.

Tong Y, Stewart KD, Florjancic AS, Harlan JE, Merta PJ, Przytulinska M, Soni N, Swinger KK, Zhu H, Johnson EF, Shoemaker AR, Penning TD.

ACS Med Chem Lett. 2013 Jan 15;4(2):211-5. doi: 10.1021/ml300348c. eCollection 2013 Feb 14.

3.

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
4.

PARP inhibitors attenuate chemotherapy-induced painful neuropathy.

Brederson JD, Joshi SK, Browman KE, Mikusa J, Zhong C, Gauvin D, Liu X, Shi Y, Penning TD, Shoemaker AR, Giranda VL.

J Peripher Nerv Syst. 2012 Sep;17(3):324-30. doi: 10.1111/j.1529-8027.2012.00413.x.

PMID:
22971094
5.

Discovery and SAR of orally efficacious tetrahydropyridopyridazinone PARP inhibitors for the treatment of cancer.

Zhu GD, Gong J, Gandhi VB, Liu X, Shi Y, Johnson EF, Donawho CK, Ellis PA, Bouska JJ, Osterling DJ, Olson AM, Park C, Luo Y, Shoemaker A, Giranda VL, Penning TD.

Bioorg Med Chem. 2012 Aug 1;20(15):4635-45. doi: 10.1016/j.bmc.2012.06.021. Epub 2012 Jun 19.

PMID:
22766219
6.

Aminopyrimidinone cdc7 kinase inhibitors.

Woods KW, Lai C, Miyashiro JM, Tong Y, Florjancic AS, Han EK, Soni N, Shi Y, Lasko L, Leverson JD, Johnson EF, Shoemaker AR, Penning TD.

Bioorg Med Chem Lett. 2012 Mar 1;22(5):1940-3. doi: 10.1016/j.bmcl.2012.01.041. Epub 2012 Jan 25.

PMID:
22326396
7.

Iniparib nonselectively modifies cysteine-containing proteins in tumor cells and is not a bona fide PARP inhibitor.

Liu X, Shi Y, Maag DX, Palma JP, Patterson MJ, Ellis PA, Surber BW, Ready DB, Soni NB, Ladror US, Xu AJ, Iyer R, Harlan JE, Solomon LR, Donawho CK, Penning TD, Johnson EF, Shoemaker AR.

Clin Cancer Res. 2012 Jan 15;18(2):510-23. doi: 10.1158/1078-0432.CCR-11-1973. Epub 2011 Nov 29.

8.

Small-molecule PARP modulators--current status and future therapeutic potential.

Penning TD.

Curr Opin Drug Discov Devel. 2010 Sep;13(5):577-86. Review.

PMID:
20812149
9.

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
10.

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
11.

ABT-888 confers broad in vivo activity in combination with temozolomide in diverse tumors.

Palma JP, Wang YC, Rodriguez LE, Montgomery D, Ellis PA, Bukofzer G, Niquette A, Liu X, Shi Y, Lasko L, Zhu GD, Penning TD, Giranda VL, Rosenberg SH, Frost DJ, Donawho CK.

Clin Cancer Res. 2009 Dec 1;15(23):7277-90. doi: 10.1158/1078-0432.CCR-09-1245. Epub 2009 Nov 24.

12.

Synthesis and evaluation of a new generation of orally efficacious benzimidazole-based poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors as anticancer agents.

Tong Y, Bouska JJ, Ellis PA, Johnson EF, Leverson J, Liu X, Marcotte PA, Olson AM, Osterling DJ, Przytulinska M, Rodriguez LE, Shi Y, Soni N, Stavropoulos J, Thomas S, Donawho CK, Frost DJ, Luo Y, Giranda VL, Penning TD.

J Med Chem. 2009 Nov 12;52(21):6803-13. doi: 10.1021/jm900697r.

PMID:
19888760
13.

Discovery of 3H-benzo[4,5]thieno[3,2-d]pyrimidin-4-ones as potent, highly selective, and orally bioavailable inhibitors of the human protooncogene proviral insertion site in moloney murine leukemia virus (PIM) kinases.

Tao ZF, Hasvold LA, Leverson JD, Han EK, Guan R, Johnson EF, Stoll VS, Stewart KD, Stamper G, Soni N, Bouska JJ, Luo Y, Sowin TJ, Lin NH, Giranda VS, Rosenberg SH, Penning TD.

J Med Chem. 2009 Nov 12;52(21):6621-36. doi: 10.1021/jm900943h.

PMID:
19842661
14.

Synthesis and SAR of novel tricyclic quinoxalinone inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1).

Miyashiro J, Woods KW, Park CH, Liu X, Shi Y, Johnson EF, Bouska JJ, Olson AM, Luo Y, Fry EH, Giranda VL, Penning TD.

Bioorg Med Chem Lett. 2009 Aug 1;19(15):4050-4. doi: 10.1016/j.bmcl.2009.06.016. Epub 2009 Jun 13.

PMID:
19553114
15.

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
16.

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.

17.

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
18.

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
19.

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
20.

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
21.

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.

22.

Synthesis of pyrazoles and isoxazoles as potent alpha(v)beta3 receptor antagonists.

Penning TD, Khilevich A, Chen BB, Russell MA, Boys ML, Wang Y, Duffin T, Engleman VW, Finn MB, Freeman SK, Hanneke ML, Keene JL, Klover JA, Nickols GA, Nickols MA, Rader RK, Settle SL, Shannon KE, Steininger CN, Westlin MM, Westlin WF.

Bioorg Med Chem Lett. 2006 Jun 15;16(12):3156-61. Epub 2006 Apr 18.

PMID:
16621534
23.

Synthesis of 2,5-thiazole butanoic acids as potent and selective alpha(v)beta3 integrin receptor antagonists with improved oral pharmacokinetic properties.

Wendt JA, Wu H, Stenmark HG, Boys ML, Downs VL, Penning TD, Chen BB, Wang Y, Duffin T, Finn MB, Keene JL, Engleman VW, Freeman SK, Hanneke ML, Shannon KE, Nickols MA, Steininger CN, Westlin M, Klover JA, Westlin W, Nickols GA, Russell MA.

Bioorg Med Chem Lett. 2006 Feb 15;16(4):845-9. Epub 2005 Nov 21.

PMID:
16303301
24.

Convergent, parallel synthesis of a series of beta-substituted 1,2,4-oxadiazole butanoic acids as potent and selective alpha(v)beta3 receptor antagonists.

Boys ML, Schretzman LA, Chandrakumar NS, Tollefson MB, Mohler SB, Downs VL, Penning TD, Russell MA, Wendt JA, Chen BB, Stenmark HG, Wu H, Spangler DP, Clare M, Desai BN, Khanna IK, Nguyen MN, Duffin T, Engleman VW, Finn MB, Freeman SK, Hanneke ML, Keene JL, Klover JA, Nickols GA, Nickols MA, Steininger CN, Westlin M, Westlin W, Yu YX, Wang Y, Dalton CR, Norring SA.

Bioorg Med Chem Lett. 2006 Feb 15;16(4):839-44. Epub 2005 Nov 17.

PMID:
16298127
25.

Synthesis of cinnamic acids and related isosteres as potent and selective alpha v beta 3 receptor antagonists.

Penning TD, Russell MA, Chen BB, Chen HY, Desai BN, Docter SH, Edwards DJ, Gesicki GJ, Liang CD, Malecha JW, Yu SS, Engleman VW, Freeman SK, Hanneke ML, Shannon KE, Westlin MM, Nickols GA.

Bioorg Med Chem Lett. 2004 Mar 22;14(6):1471-6.

PMID:
15006384
26.

Synthesis of imidazopyridines and purines as potent inhibitors of leukotriene A4 hydrolase.

Penning TD, Chandrakumar NS, Desai BN, Djuric SW, Gasiecki AF, Malecha JW, Miyashiro JM, Russell MA, Askonas LJ, Gierse JK, Harding EI, Highkin MK, Kachur JF, Kim SH, Villani-Price D, Pyla EY, Ghoreishi-Haack NS, Smith WG.

Bioorg Med Chem Lett. 2003 Mar 24;13(6):1137-9.

PMID:
12643929
27.

Pyrrolidine and piperidine analogues of SC-57461A as potent, orally active inhibitors of leukotriene A(4) hydrolase.

Penning TD, Chandrakumar NS, Desai BN, Djuric SW, Gasiecki AF, Liang CD, Miyashiro JM, Russell MA, Askonas LJ, Gierse JK, Harding EI, Highkin MK, Kachur JF, Kim SH, Villani-Price D, Pyla EY, Ghoreishi-Haack NS, Smith WG.

Bioorg Med Chem Lett. 2002 Dec 2;12(23):3383-6.

PMID:
12419366
28.

Synthesis of potent leukotriene A(4) hydrolase inhibitors. Identification of 3-[methyl[3-[4-(phenylmethyl)phenoxy]propyl]amino]propanoic acid.

Penning TD, Russell MA, Chen BB, Chen HY, Liang CD, Mahoney MW, Malecha JW, Miyashiro JM, Yu SS, Askonas LJ, Gierse JK, Harding EI, Highkin MK, Kachur JF, Kim SH, Villani-Price D, Pyla EY, Ghoreishi-Haack NS, Smith WG.

J Med Chem. 2002 Aug 1;45(16):3482-90.

PMID:
12139459
29.

Inhibitors of leukotriene A4 (LTA4) hydrolase as potential anti-inflammatory agents.

Penning TD.

Curr Pharm Des. 2001 Feb;7(3):163-79. Review.

PMID:
11311111
30.

Structure-activity relationship studies on 1-[2-(4-Phenylphenoxy)ethyl]pyrrolidine (SC-22716), a potent inhibitor of leukotriene A(4) (LTA(4)) hydrolase.

Penning TD, Chandrakumar NS, Chen BB, Chen HY, Desai BN, Djuric SW, Docter SH, Gasiecki AF, Haack RA, Miyashiro JM, Russell MA, Yu SS, Corley DG, Durley RC, Kilpatrick BF, Parnas BL, Askonas LJ, Gierse JK, Harding EI, Highkin MK, Kachur JF, Kim SH, Krivi GG, Villani-Price D, Pyla EY, Smith WG.

J Med Chem. 2000 Feb 24;43(4):721-35.

PMID:
10691697
31.

Synthesis and biological evaluation of the 1,5-diarylpyrazole class of cyclooxygenase-2 inhibitors: identification of 4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benze nesulfonamide (SC-58635, celecoxib).

Penning TD, Talley JJ, Bertenshaw SR, Carter JS, Collins PW, Docter S, Graneto MJ, Lee LF, Malecha JW, Miyashiro JM, Rogers RS, Rogier DJ, Yu SS, AndersonGD, Burton EG, Cogburn JN, Gregory SA, Koboldt CM, Perkins WE, Seibert K, Veenhuizen AW, Zhang YY, Isakson PC.

J Med Chem. 1997 Apr 25;40(9):1347-65.

PMID:
9135032
32.

Structural basis for selective inhibition of cyclooxygenase-2 by anti-inflammatory agents.

Kurumbail RG, Stevens AM, Gierse JK, McDonald JJ, Stegeman RA, Pak JY, Gildehaus D, Miyashiro JM, Penning TD, Seibert K, Isakson PC, Stallings WC.

Nature. 1996 Dec 19-26;384(6610):644-8. Erratum in: Nature 1997 Feb 6;385(6616):555.

PMID:
8967954
33.

Antiinflammatory effects of second-generation leukotriene B4 receptor antagonist, SC-53228: impact upon leukotriene B4- and 12(R)-HETE-mediated events.

Fretland DJ, Anglin CP, Bremer M, Isakson P, Widomski DL, Paulson SK, Docter SH, Djuric SW, Penning TD, Yu S, et al.

Inflammation. 1995 Apr;19(2):193-205.

PMID:
7601505
34.

Second-generation leukotriene B4 receptor antagonists related to SC-41930: heterocyclic replacement of the methyl ketone pharmacophore.

Penning TD, Djuric SW, Miyashiro JM, Yu S, Snyder JP, Spangler D, Anglin CP, Fretland DJ, Kachur JF, Keith RH, et al.

J Med Chem. 1995 Mar 17;38(6):858-68.

PMID:
7699700
35.

Leukotriene B4-induced granulocyte trafficking in guinea pig dermis. Effect of second-generation leukotriene B4 receptor antagonists, SC-50605 and SC-51146.

Fretland DJ, Widomski DL, Anglin CP, Penning TD, Yu S, Djuric SW.

Inflammation. 1993 Jun;17(3):353-60.

PMID:
8392493
36.

The design and synthesis of second generation leukotriene B4 (LTB4) receptor antagonists related to SC-41930.

Penning TD, Djuric SW, Docter SH, Yu SS, Spangler D, Anglin CP, Fretland DJ, Kachur JF, Keith RH, Tsai BS, et al.

Agents Actions. 1993;39 Spec No:C11-3.

PMID:
8273545
37.

SC-41930 inhibits neutrophil infiltration of the cavine dermis induced by 12(R)-hydroxyeicosatetraenoic acid.

Fretland DJ, Widomski DL, Shone RL, Penning TD, Miyashiro JM, Djuric SW.

Prostaglandins Leukot Essent Fatty Acids. 1989 Dec;38(3):169-72.

PMID:
2560200
38.

12(R)-hydroxyeicosatetraenoic acid is a neutrophil chemoattractant in the cavine, lapine, murine and canine dermis.

Fretland DJ, Widomski DL, Zemaitis JM, Tsai BS, Djuric SW, Penning TD, Miyashiro JM, Bauer RF.

Prostaglandins Leukot Essent Fatty Acids. 1989 Aug;37(2):79-81.

PMID:
2550970

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