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Items: 39

1.

Preclinical characterization of ABT-348, a kinase inhibitor targeting the aurora, vascular endothelial growth factor receptor/platelet-derived growth factor receptor, and Src kinase families.

Glaser KB, Li J, Marcotte PA, Magoc TJ, Guo J, Reuter DR, Tapang P, Wei RQ, Pease LJ, Bui MH, Chen Z, Frey RR, Johnson EF, Osterling DJ, Olson AM, Bouska JJ, Luo Y, Curtin ML, Donawho CK, Michaelides MR, Tse C, Davidsen SK, Albert DH.

J Pharmacol Exp Ther. 2012 Dec;343(3):617-27. doi: 10.1124/jpet.112.197087. Epub 2012 Aug 30.

PMID:
22935731
2.

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
3.

Exploration of diverse hinge-binding scaffolds for selective Aurora kinase inhibitors.

Ji Z, Dai Y, Abad-Zapatero C, Albert DH, Bouska JJ, Glaser KB, Marcotte PA, Soni NB, Magoc TJ, Stewart KD, Wei RQ, Davidsen SK, Michaelides MR.

Bioorg Med Chem Lett. 2012 Jul 15;22(14):4528-31. doi: 10.1016/j.bmcl.2012.05.125. Epub 2012 Jun 7.

PMID:
22727637
4.

Pyrazole diaminopyrimidines as dual inhibitors of KDR and Aurora B kinases.

Curtin ML, Heyman HR, Frey RR, Marcotte PA, Glaser KB, Jankowski JR, Magoc TJ, Albert DH, Olson AM, Reuter DR, Bouska JJ, Montgomery DA, Palma JP, Donawho CK, Stewart KD, Tse C, Michaelides MR.

Bioorg Med Chem Lett. 2012 Jul 15;22(14):4750-5. doi: 10.1016/j.bmcl.2012.05.067. Epub 2012 May 26.

PMID:
22695126
5.

Thienopyridine ureas as dual inhibitors of the VEGF and Aurora kinase families.

Curtin ML, Frey RR, Heyman HR, Soni NB, Marcotte PA, Pease LJ, Glaser KB, Magoc TJ, Tapang P, Albert DH, Osterling DJ, Olson AM, Bouska JJ, Guan Z, Preusser LC, Polakowski JS, Stewart KD, Tse C, Davidsen SK, Michaelides MR.

Bioorg Med Chem Lett. 2012 May 1;22(9):3208-12. doi: 10.1016/j.bmcl.2012.03.035. Epub 2012 Mar 14.

PMID:
22465635
6.

Discovery of potent and selective thienopyrimidine inhibitors of Aurora kinases.

McClellan WJ, Dai Y, Abad-Zapatero C, Albert DH, Bouska JJ, Glaser KB, Magoc TJ, Marcotte PA, Osterling DJ, Stewart KD, Davidsen SK, Michaelides MR.

Bioorg Med Chem Lett. 2011 Sep 15;21(18):5620-4. doi: 10.1016/j.bmcl.2011.06.041. Epub 2011 Jun 29.

PMID:
21778056
7.

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
8.

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
9.

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
10.

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
11.

Identification of genes that confer tumor cell resistance to the aurora B kinase inhibitor, AZD1152.

Guo J, Anderson MG, Tapang P, Palma JP, Rodriguez LE, Niquette A, Li J, Bouska JJ, Wang G, Semizarov D, Albert DH, Donawho CK, Glaser KB, Shah OJ.

Pharmacogenomics J. 2009 Apr;9(2):90-102. doi: 10.1038/tpj.2008.20. Epub 2009 Feb 3.

PMID:
19188929
12.

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
13.

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.

14.

7-Aminopyrazolo[1,5-a]pyrimidines as potent multitargeted receptor tyrosine kinase inhibitors.

Frey RR, Curtin ML, Albert DH, Glaser KB, Pease LJ, Soni NB, Bouska JJ, Reuter D, Stewart KD, Marcotte P, Bukofzer G, Li J, Davidsen SK, Michaelides MR.

J Med Chem. 2008 Jul 10;51(13):3777-87. doi: 10.1021/jm701397k. Epub 2008 Jun 17.

PMID:
18557606
15.

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
16.

3-amino-benzo[d]isoxazoles as novel multitargeted inhibitors of receptor tyrosine kinases.

Ji Z, Ahmed AA, Albert DH, Bouska JJ, Bousquet PF, Cunha GA, Diaz G, Glaser KB, Guo J, Harris CM, Li J, Marcotte PA, Moskey MD, Oie T, Pease L, Soni NB, Stewart KD, Davidsen SK, Michaelides MR.

J Med Chem. 2008 Mar 13;51(5):1231-41. doi: 10.1021/jm701096v. Epub 2008 Feb 9.

PMID:
18260617
17.

Identification of aminopyrazolopyridine ureas as potent VEGFR/PDGFR multitargeted kinase inhibitors.

Dai Y, Hartandi K, Soni NB, Pease LJ, Reuter DR, Olson AM, Osterling DJ, Doktor SZ, Albert DH, Bouska JJ, Glaser KB, Marcotte PA, Stewart KD, Davidsen SK, Michaelides MR.

Bioorg Med Chem Lett. 2008 Jan 1;18(1):386-90. Epub 2007 Oct 17.

PMID:
18023347
18.

Design, synthesis, and biological activity of 5,10-dihydro-dibenzo[b,e][1,4]diazepin-11-one-based potent and selective Chk-1 inhibitors.

Wang L, Sullivan GM, Hexamer LA, Hasvold LA, Thalji R, Przytulinska M, Tao ZF, Li G, Chen Z, Xiao Z, Gu WZ, Xue J, Bui MH, Merta P, Kovar P, Bouska JJ, Zhang H, Park C, Stewart KD, Sham HL, Sowin TJ, Rosenberg SH, Lin NH.

J Med Chem. 2007 Aug 23;50(17):4162-76. Epub 2007 Jul 21.

PMID:
17658776
19.

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.

20.

1,4-Dihydroindeno[1,2-c]pyrazoles with acetylenic side chains as novel and potent multitargeted receptor tyrosine kinase inhibitors with low affinity for the hERG ion channel.

Dinges J, Albert DH, Arnold LD, Ashworth KL, Akritopoulou-Zanze I, Bousquet PF, Bouska JJ, Cunha GA, Davidsen SK, Diaz GJ, Djuric SW, Gasiecki AF, Gintant GA, Gracias VJ, Harris CM, Houseman KA, Hutchins CW, Johnson EF, Li H, Marcotte PA, Martin RL, Michaelides MR, Nyein M, Sowin TJ, Su Z, Tapang PH, Xia Z, Zhang HQ.

J Med Chem. 2007 May 3;50(9):2011-29. Epub 2007 Apr 11.

PMID:
17425296
21.

Discovery of N-(4-(3-amino-1H-indazol-4-yl)phenyl)-N'-(2-fluoro-5-methylphenyl)urea (ABT-869), a 3-aminoindazole-based orally active multitargeted receptor tyrosine kinase inhibitor.

Dai Y, Hartandi K, Ji Z, Ahmed AA, Albert DH, Bauch JL, Bouska JJ, Bousquet PF, Cunha GA, Glaser KB, Harris CM, Hickman D, Guo J, Li J, Marcotte PA, Marsh KC, Moskey MD, Martin RL, Olson AM, Osterling DJ, Pease LJ, Soni NB, Stewart KD, Stoll VS, Tapang P, Reuter DR, Davidsen SK, Michaelides MR.

J Med Chem. 2007 Apr 5;50(7):1584-97. Epub 2007 Mar 8.

PMID:
17343372
22.

ABT-869, a multitargeted receptor tyrosine kinase inhibitor: inhibition of FLT3 phosphorylation and signaling in acute myeloid leukemia.

Shankar DB, Li J, Tapang P, Owen McCall J, Pease LJ, Dai Y, Wei RQ, Albert DH, Bouska JJ, Osterling DJ, Guo J, Marcotte PA, Johnson EF, Soni N, Hartandi K, Michaelides MR, Davidsen SK, Priceman SJ, Chang JC, Rhodes K, Shah N, Moore TB, Sakamoto KM, Glaser KB.

Blood. 2007 Apr 15;109(8):3400-8. Epub 2007 Jan 5.

23.

Thienopyridine urea inhibitors of KDR kinase.

Heyman HR, Frey RR, Bousquet PF, Cunha GA, Moskey MD, Ahmed AA, Soni NB, Marcotte PA, Pease LJ, Glaser KB, Yates M, Bouska JJ, Albert DH, Black-Schaefer CL, Dandliker PJ, Stewart KD, Rafferty P, Davidsen SK, Michaelides MR, Curtin ML.

Bioorg Med Chem Lett. 2007 Mar 1;17(5):1246-9. Epub 2006 Dec 9.

PMID:
17188869
24.

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
25.

Isothiazolopyrimidines and isoxazolopyrimidines as novel multi-targeted inhibitors of receptor tyrosine kinases.

Ji Z, Ahmed AA, Albert DH, Bouska JJ, Bousquet PF, Cunha GA, Glaser KB, Guo J, Li J, Marcotte PA, Moskey MD, Pease LJ, Stewart KD, Yates M, Davidsen SK, Michaelides MR.

Bioorg Med Chem Lett. 2006 Aug 15;16(16):4326-30. Epub 2006 Jun 2.

PMID:
16735117
26.

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
27.

Preclinical activity of ABT-869, a multitargeted receptor tyrosine kinase inhibitor.

Albert DH, Tapang P, Magoc TJ, Pease LJ, Reuter DR, Wei RQ, Li J, Guo J, Bousquet PF, Ghoreishi-Haack NS, Wang B, Bukofzer GT, Wang YC, Stavropoulos JA, Hartandi K, Niquette AL, Soni N, Johnson EF, McCall JO, Bouska JJ, Luo Y, Donawho CK, Dai Y, Marcotte PA, Glaser KB, Michaelides MR, Davidsen SK.

Mol Cancer Ther. 2006 Apr;5(4):995-1006.

28.

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
29.

Thienopyrimidine ureas as novel and potent multitargeted receptor tyrosine kinase inhibitors.

Dai Y, Guo Y, Frey RR, Ji Z, Curtin ML, Ahmed AA, Albert DH, Arnold L, Arries SS, Barlozzari T, Bauch JL, Bouska JJ, Bousquet PF, Cunha GA, Glaser KB, Guo J, Li J, Marcotte PA, Marsh KC, Moskey MD, Pease LJ, Stewart KD, Stoll VS, Tapang P, Wishart N, Davidsen SK, Michaelides MR.

J Med Chem. 2005 Sep 22;48(19):6066-83.

PMID:
16162008
30.

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.

31.

Heterocyclic ketones as inhibitors of histone deacetylase.

Vasudevan A, Ji Z, Frey RR, Wada CK, Steinman D, Heyman HR, Guo Y, Curtin ML, Guo J, Li J, Pease L, Glaser KB, Marcotte PA, Bouska JJ, Davidsen SK, Michaelides MR.

Bioorg Med Chem Lett. 2003 Nov 17;13(22):3909-13.

PMID:
14592473
32.

Alpha-keto amides as inhibitors of histone deacetylase.

Wada CK, Frey RR, Ji Z, Curtin ML, Garland RB, Holms JH, Li J, Pease LJ, Guo J, Glaser KB, Marcotte PA, Richardson PL, Murphy SS, Bouska JJ, Tapang P, Magoc TJ, Albert DH, Davidsen SK, Michaelides MR.

Bioorg Med Chem Lett. 2003 Oct 6;13(19):3331-5.

PMID:
12951120
33.

Trifluoromethyl ketones as inhibitors of histone deacetylase.

Frey RR, Wada CK, Garland RB, Curtin ML, Michaelides MR, Li J, Pease LJ, Glaser KB, Marcotte PA, Bouska JJ, Murphy SS, Davidsen SK.

Bioorg Med Chem Lett. 2002 Dec 2;12(23):3443-7.

PMID:
12419380
34.

Phenoxyphenyl sulfone N-formylhydroxylamines (retrohydroxamates) as potent, selective, orally bioavailable matrix metalloproteinase inhibitors.

Wada CK, Holms JH, Curtin ML, Dai Y, Florjancic AS, Garland RB, Guo Y, Heyman HR, Stacey JR, Steinman DH, Albert DH, Bouska JJ, Elmore IN, Goodfellow CL, Marcotte PA, Tapang P, Morgan DW, Michaelides MR, Davidsen SK.

J Med Chem. 2002 Jan 3;45(1):219-32.

PMID:
11754593
35.

Discovery and characterization of the potent, selective and orally bioavailable MMP inhibitor ABT-770.

Curtin ML, Florjancic AS, Heyman HR, Michaelides MR, Garland RB, Holms JH, Steinman DH, Dellaria JF, Gong J, Wada CK, Guo Y, Elmore IB, Tapang P, Albert DH, Magoc TJ, Marcotte PA, Bouska JJ, Goodfellow CL, Bauch JL, Marsh KC, Morgan DW, Davidsen SK.

Bioorg Med Chem Lett. 2001 Jun 18;11(12):1557-60.

PMID:
11412980
36.

Biaryl ether retrohydroxamates as potent, long-lived, orally bioavailable MMP inhibitors.

Michaelides MR, Dellaria JF, Gong J, Holms JH, Bouska JJ, Stacey J, Wada CK, Heyman HR, Curtin ML, Guo Y, Goodfellow CL, Elmore IB, Albert DH, Magoc TJ, Marcotte PA, Morgan DW, Davidsen SK.

Bioorg Med Chem Lett. 2001 Jun 18;11(12):1553-6.

PMID:
11412979
37.

Discovering novel ligands for macromolecules using X-ray crystallographic screening.

Nienaber VL, Richardson PL, Klighofer V, Bouska JJ, Giranda VL, Greer J.

Nat Biotechnol. 2000 Oct;18(10):1105-8.

PMID:
11017052
38.

Aryl ketones as novel replacements for the C-terminal amide bond of succinyl hydroxamate MMP inhibitors.

Sheppard GS, Florjancic AS, Giesler JR, Xu L, Guo Y, Davidsen SK, Marcotte PA, Elmore I, Albert DH, Magoc TJ, Bouska JJ, Goodfellow CL, Morgan DW, Summers JB.

Bioorg Med Chem Lett. 1998 Nov 17;8(22):3251-6.

PMID:
9873712
39.

Improving the in vivo duration of 5-lipoxygenase inhibitors: application of an in vitro glucuronosyltransferase assay.

Bouska JJ, Bell RL, Goodfellow CL, Stewart AO, Brooks CD, Carter GW.

Drug Metab Dispos. 1997 Sep;25(9):1032-8.

PMID:
9311617

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